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SML2830 trans-Ned-19 ≥98% (HPLC) New NAADP (nicotinic acid adenine dinucleotide phosphate) has recently been recognized as a crucial Ca2+-releasing second messenger in several mammalian tissues including pancreatic, brain and cardiac. Ned-19 is a potent inhibitor of NAADP action. It is a selective blocker of cellular NAADP-induced Ca2+-release and can fluorescently label NAADP receptors. Ned-19 blocks NAADP signaling at nanomolar concentrations. In intact cells, Ned-19 blocked NAADP signaling and fluorescently labeled NAADP receptors.The trans-Ned-19 is more potent than the cis form in regard to both inhibition of Ca2+ release (IC50 of 6 nM versus 800 nM) and [32P]NAADP binding (IC50 of 0.4 nM versus 15 μM).
SML1915 T-26c ≥98% (HPLC) T-26c is a highly potent, selective and cell-permeable matrix metalloproteinases 13 (MMP-13) inhibitor. T-26c inhibits the breakdown of collagen (87.4% inhibition at 0.1 μM) in IL-1b and oncostatin M stimulated cartilage. For full characterization details, please visit the T-26c probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
T8703 T0070907 ≥98% (HPLC) T0070907 is very similar in structure and activity to the PPAR-γ antagonist GW9662. T0070907 is more potent and has higher selectivity for PPAR-γ over all other subtypes (about 800-fold) whereas GW9662 has been reported to have some PPAR-α agonist activity.
SML0493 T16Ainh-A01 ≥95% (HPLC) T16Ainh-A01 is a selective TMEM16A calcium-activated chloride channel inhibitor that strongly inhibits chloride current in salivary gland cells. T16Ainh-A01 poorly inhibited total CaCC current in intestinal and airway epithelial cells, but blocked mainly an initial, agonist-stimulated transient chloride current. T16Ainh-A01 does not alter cytoplasmic calcium and has little effect on CFTR Cl- conductance.
SML1924 T1AM ≥98% (HPLC) T1AM (3-Iodothyronamine) is an endogenous biogenic amine derived from thyroid hormone. T1AM is a potent agonist of trace amine-associated receptor TAAR1 (TAR1, TA1), a GPCR primarily found in the brain.
SML0794   T2AA hydrochloride ≥98% (HPLC) T2AA is an inhibitor of PCNA/ PIP-Box interactions that binds to the PCNA cavity that interacts with PIP-Box sequences. Also T2AA inhibits PCNA Polδ3 interaction. T2AA inhibits de novo DNA synthesis, and in combination of cisplatin significantly increases growth inhibition in cancer cells. T2AA is a T3 analog that exhibits almost no thyroid hormone activity.
SML2650 T3-CLK ≥98% (HPLC) New T3-CLK (T3) is a cell permeable, highly potent and selective cell-base stable inhibitor of CDC-like kinase (CLK) that exhibits dose-dependent alternative splicing effects in HCT116 colorectal cancer cells. T3-CLK increases conjoined gene (CG) transcription.
SML2649 T3-CLK-N ≥98% (HPLC) New T3-CLK-N (T3N) is a negative control for CDC-like kinase (CLK) inhibitor T3-CLK.
T2455 T3MG T3MG is a selective inhibitor of excitatory amino acid transporters GLT-1, EAAT2, and EAAT4. T3MG has long been utilized as a gold standard in the study of general EAAT function. It has more recently been shown to be selective for EAAT2 and EAAT4 as compared to EAAT1 and EAAT3 in electrophysiology and glutamate/aspartate uptake assays. Although there are other EAAT2-selective compounds, this is the first tool with selectivity for EAAT4. T3MG is not a substrate for the transporters themselves, nor does it have activity at glutamate ion channels.
SML1305 T56-LIMKi ≥98% (HPLC) T56-LIMKi is a LIMK2 inhibitor that reduces phosphorylated cofilin, and induces disassembly of actin stress fibers in NF1-/- MEFs cells.
T7450 T62 ≥98% (HPLC), crystalline Allosteric enhancer of A1 adenosine receptor.
Studies in carrageenin-inflamed rats have reported that T62 can reverse thermal hypersensitivity. T62 has also been reported to reduce mechanical allodynia and induce drug tolerance over time in rat models of neuropathic pain.
human ... ADORA1(134)
SML0539 T863 ≥98% (HPLC) T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells. T863 causes weight loss, reduction in serum and liver triglycerides, and improved insulin sensitivity in obese mice.
SML1877 Tadalafil ≥98% (HPLC) Tadalafil is a potent, selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5) used to treat erectile dysfunction, pulmonary hypertension, and benign prostatic hyperplasia (BPH).
This β-carboline-based drug has a long elimination half-life of about 18 hours.
SML0967   TAE-1 ≥98% (HPLC) TAE-1 is an inhibitor of amyloid-β fibril formation and aggregation. TAE-1 is a sym-triazine with dual activity against Alzheimer′s disease. TAE-1 inhibits cholinesterases AChE and BuChE with IC50 values of 0.3 and 3.9 μM. Studies using TAE-1 on differentiated human SH-SY5Y neuronal cells have suggested that it can stimulate synapse formation and promote the differentiation of human neurons, increasing neurite extension.
SML0396 Tafenoquine succinate ≥95% (HPLC) Tafenoquine has been generally generated for oral administration and drug absorption increases when taken along with food. It is known to possess a longer half life.
Tafenoquine is an antimalarial primaquine analog being investigated to treat and prevent Plasmodium vivax infections. It can eliminate both blood and liver stages of Plasmodium vivax. Tafenoquine has also been tested as a therapy for leishmaniasis.
SML2525 Tafluprost ≥98% (HPLC) Taflupost is a prostaglandin F2α agonist that lowers intraocular pressure and is used in the treatment of glaucoma. It has high affinity and selectivity for the fluoroprostaglandin (FP) receptor PGF2α. Tafluprost is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Tafluprost is a pro-drug. The active metabolite is the free acid.
SML2579 Tafluprost acid ≥98% (HPLC) Taflupost acid is the active metabolite of Tafluprost, a prostaglandin F2α agonist that lowers intraocular pressure and is used in the treatment of glaucoma. Taflupost acid has high affinity and selectivity for the prostaglandin PGF2α (FP) receptor with a Ki of 0.4 nM.
SML2168 TAK-475 ≥98% (HPLC) TAK-475 (Lapaquistat acetate) is a potent and selective squalene synthase inhibitor. TAK-475 effectively lowers low-density lipoprotein cholesterol in human. Clinical development of TAK-475 was discontinued due to hepatotoxicity seen in two patients receiving a high dose.
SML0360 TAK-715 ≥98% (HPLC) TAK-715 is a potent p38 inhibitor that also inhibits CKId/e (casein kinase Id/e), known activator of Wnt/β-catenin signaling.
human ... MAPK14(1432)
SML0911   TAK-779 ≥98% (HPLC) TAK-779 is a potent, dual antagonist at chemokine receptors CCR2 and CCR5 with IC50 = 1.4 nM at CCR5 and 2.3 nM at CCR2. Antagonists of both CCR2 and CCR5 such as TAK-779 have been investigated for treatment of viruses, rheumatoid arthritis, multiple sclerosis, and cancer. CCR5 is particularly targeted for anti-HIV therapy, since HIV entry into cells requires chemokine coreceptors CCR5 and CXCR4.
SML2155 TAK-901 ≥98% (HPLC) TAK-901 is a potent and tight-binding Aurora B kinase inhibitor. TAK-901 targets multiple kinases in vitro, but appears to mainly target Aurora B in cells and in vivo. TAK-901 suppresses cellular histone H3 phosphorylation and induced polyploidy.
SML2216 Takinib ≥98% (HPLC) Takinib is a selective inhibitor of TAK1/MAP3K7 kinase, which is a member of the MAP3K family and a key regulator of cell death. It binds in the TAk1 ATPbinding pocket with an IC50 value of 9.5 nM. Takinib selectively induced apoptosis following TNF-α stimulation in rheumatoid arthritis and breast cancer.
SML0686 Talampanel ≥97% (HPLC) Talampanel ia a specific noncompetitive AMPA receptor antagonist and anticonvulsant.
SML1165 Talnetant ≥98% (HPLC) Talnetant (SB-223,412) is a highly selective antagonist of neurokinin 3 receptor with a Ki (NK3) = 1 nM >10000 (NK1) >140 (NK2). Neurokinins (tachykinins) are members of a family of at least three neuropeptides, substance P, neurokinin A, and neurokinin B (NKB), with each mediating their biological effects through binding to a preferred G-protein-coupled receptor termed NK1, NK2, or NK3, respectively. All three NK receptors are expressed in regions of the central nervous system that are related to emotion and cognition (i.e., amygdala and hippocampus) and have been linked to various degrees in psychiatric disorders. Neurokinin receptors, including NK3 receptors, are also expressed in the motor and sensory systems of the digestive tract. Talnetant was in clinical trials for both irritable bowel syndrome and schizophrenia.
human ... TACR3(6870)
SML1710   Talniflumate ≥98% (HPLC) Talniflumate is a phthalidyl ester of niflumic acid. It acts as an anti-inflammatory molecule and a mucoregulator. Talniflumate is used as a potent therapeutic for cystic fibrosis, chronic obstructive pulmonary disease and asthma. Talniflumate also inhibits the calcium-activated chloride channel hCLCA function, which is involved in mucus overproduction.
Talniflumate is an orally available, potent and selective inhibitor of core mucin-synthesizing enzyme GCNT3 (core 2 b-1,6 N-acetylglucosaminyltransferase). Talniflumate decreases GCNT3 expression and production of mucins in vivo and in vitro. Talniflumate improves responsiveness of pancreatic tumors to gefitinib. Talniflumate is a potent calcium-activated chloride channel (CaCC) blocker.
T2452 Talsaclidine ≥98% (HPLC), oil Talsaclidine is a M1 selective muscarinic receptor agonist. Concentration-dependently, talsaclidine increases the release of APPs and dose-dependently. Talsaclidine decreases Aβ formation and decreases cerebrospinal fluid Aβ in AD patients.
SML2153 TAM1 hydrochloride ≥98% (HPLC) TAM1 is an inhibitor of the thioesterase activity of Mycobacterium tuberculosis polyketide synthase Pks13. TAM1 binds to Pks13 TE domain. TAM1 exhibit a potent bactericidal activity against Mycobacterium Tuberculosis H37Rv strain.
T3326   Tamapin recombinant, expressed in E. coli, ≥95% (HPLC), lyophilized powder Member of the α-5.4 scorpion toxin family. Blocks KCa2 channels with selectivity for KCa2.2 versus KCa2.1 channels.
Tamapin strongly associates with Ca(2+)-activated K(+) (SK) channels and blocks SK-channel mediated currents in hippocampal neurons1.
T3205 Tamibarotene ≥98% (HPLC) Tamibarotene (Am80) is a RAR α agonist. Tamibarotene was developed to overcome resistance to ATRA and is currently approved in Japan for treatment of recurrent acute promyelocytic leukemia (APL). The compound induces HL-60 cells differentiation and apoptosis. Similarly to TTNPB, the compound neither binds to nor transactivates the RXRs. In contrast to TTNPB (pan RAR agonist), Tamibarotene is rather specific toward RAR α. The compound is approximate 10 times more potent than ATRA.
Tamibarotene is a synthetic retinoid drug, highly stable and potent inducer of differentiation than ATRA (all-trans retinoic acid). It showed mild growth inhibition in myeloma cells and HUVECs (human umbilical vein endothelial cell).
T5648 Tamoxifen ≥99% Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
human ... CYP1A2(1544), EBP(10682), ESR1(2099), ESR2(2100), ESRRA(2101)
rat ... Ar(24208), Esr1(24890)
T9262 Tamoxifen citrate salt ≥99% Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells.
human ... ESR1(2099), PRKCA(5578), PRKCB(5579), PRKCD(5580), PRKCE(5581), PRKCG(5582), PRKCH(5583), PRKCI(5584)
T1330 Tamsulosin hydrochloride ≥98% (HPLC) Tamsulosin is an α1A/1D-adrenoceptor antagonist used as a treatment of benign prostatic hypertrophy (BPH). Its activity as an ? blocker also affects the iris, and has led to complications during cataract surgery, a condition called "floppy iris" syndrome.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
SML2779 Tanaproget ≥98% (HPLC) Tanaproget is a high affinity, high efficacy and selective orally available non-steroidal progesterone receptor agonist.
T6704 Tandospirone ≥98% (HPLC) Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner. The potency of tandospirone is equal to that of buspirone and approximate half that of diazepam. The potency of tandospirone as a dopamine antagonistic is less than 1/4 that of buspirone.
SML2672 Tandutinib hydrochloride ≥98% (HPLC) Tandutinib (CT53518, MLN518) is a potent receptor tyrosine kinase inhibitor against PDGFRβ, c-Kit, Flt3 (IC50 = 0.20, 0.17, 0.22, 3.43 μM, respectively, against 8 nM PDGF-BB induced autophosphorylation of βPDGFR, βPDGFR/c-Kit, βPDGFR/Flt3, βPDGFR/CSF-1R chimera expressed in CHO cells; IC50 =30 μM against KDR, EFGR, FGFR, InsR, Abl, Src, PKA, PKC, ERK2, MEK1, MKK4/6, p38). Tandutinib prolongs the survival in murine CMML (Baf3 with Tel/βPDGFR chimera) and Flt-3/ITD AML leukemia models (60 mg/kg bid p.o.) with good oral bioavailability.
SML2517 Tanshinone II-A sodium sulfonate ≥95% Tanshinone II A sulfonate is a water-soluble derivative of tanshinone II A that exhibits anti-inflammatory properties in rodent models of hepatitis and sepsis. Tanshinone II A sulfonate targets Ca2+-activated potassium channels and carboxylesterase 2. Recent studies indicate that tanshinone II A sulfonate but not tanshinone II A acts as potent negative allosteric modulator of the human purinergic receptor P2X7.
SML1292 TAPI-0 ≥95% (HPLC) TAPI-0 inhibit peptide deformylase (PDF) activity and retard the growth Chlamydia trachomatis, which is an obligate intracellular bacterium responsible for a number of human diseases.
TAPI-0 is a metalloproteinase inhibitor with selectivity for TACE (TNF-α converting enzyme/ADAM17; IC50 = 100 nM). TAPI-0 also inhibits of collagenase and gelatinase. Although not specific for TACE, TAPI-0 is extensively used to block TACE-mediated TNF-α shedding.
SML0739   TAPI-1 acetate salt ≥97% (HPLC) TAPI-1 is a potent inhibitor of matrix metalloproteinases and TACE (TNF-α convertase/ADAM17/α-secretase).
SML0420 TAPI-2 acetate salt ≥98% (HPLC) TAPI-2 is a potent inhibitor matrix metalloproteinases and TACE (TNF-α convertase/ADAM17/α-secretase). It blocks the shedding of several cell surface proteins such as β-amyloid precursor protein, inhibits TNF-α release as well as a diverse variety of membrane-anchored cytokines, cell adhesion molecules, receptors, ligands. TAPI-2 is considered a fairly broad metalloproteinase inhibitor, but it much more selective for TACE than GM6001.
T4949 Taprostene sodium salt ≥98% (HPLC) Highly selective IP1 prostanoid receptor agonist.
SML2841 Tarenflurbil ≥98% (HPLC) New Tarenflurbil (or R-flurbiprofen) is an R enantiomer of racemic NSAID flurbiprofen that does not inhibit either cyclooxygenase 1 (COX-1) or cyclooxygenase 2 (COX-2). Tarenflurbil potently reduces levels of beta amyloid in human cells through direct inhibition of γ-secretase.
SML1790 Tariquidar ≥98% (HPLC) Specific inhibitor of MDR-1 (P-gp)
Tariquidar is a non-competitive inhibitor. It is used as a potential agent for checking the role of P-glycoprotein inhibition in cancer. Tariquidar also has an ability to enhance drug exposure in drug-resistant cancers.
Tariquidar is a potent MDR1 (P-gp, P-glycoprotein) inhibitor. Tariquidar reverses multidrug resistance (MDR) by inhibiting MDR1-mediated drug efflux.
SML1677 Tarocin A1 ≥98% (HPLC) Tarocin A1 is an oxazolidinone which inhibits TarO, the first enzyme in teichoic acid synthesis. Tarocin A1 has an IC50 value of 40 nM in a biochemical TarO assay. Tarocin A does not inhibit bacterial growth alone, and exhibits no cytotoxicity against HeLa cells, but it has potent bactericidal syergism with broad spectrum β-lactams, and may restore the clinical efficacy of existing β-lactam antibiotics.
T9324 TAS-301 ≥95% (HPLC), solid Inhibitor of migration and proliferation in vascular smooth muscle cells; inhibitor of restenosis.
TAS-301 is known to block intimal thickening post balloon injury in rat carotid arteries. It inhibits intimal thickening by blocking Ca2+/calmodulin-dependent protein kinase II (CaM kinase II) and cytoskeletal depolymerization. Moreover, TAS 301 can also inhibit receptor-regulated influx of calcium in rat vascular smooth muscle cells (VSMCs).
SML2030 Tasimelteon ≥98% (HPLC) Tasimelteon is a Dual Melatonin Receptor Agonist (DMRA) recently approved (Hetlioz) for the treatment of Non-24-hour sleep–wake disorder, a disorder primarily found in the totally blind, where a lack of normal synchronization between the 24-hour light–dark cycle and the endogenous circadian rhythm causes it to drift out of alignment with conventional sleep–wake schedules. The endogenous rhythm of the circadian pacemaker in the suprachiasmatic nuclei (SCN) is typically slightly longer than 24 h and therefore must be synchronized to the 24-hour day, normally by light, but exogenous melatonin can also phase-shift circadian rhythms. Tasimelteon is a selective agonist for the SCN melatonin receptors MT1 and MT2 with greater affinity for the MT2 receptor thought to be more important in mediating circadian rhythm phase-shifting. EC50 values are 0.75 nM for MT1 and 0.1 nM for MT2 measured by inhibition of forskolin-stimulated cAMP accumulation in NIH-3T3 cells expressing human MT1 and MT2.
SML1988 TASIN-1 hydrochloride ≥98% (HPLC) TASIN-1 (Truncated APC Selective INhibitor-1) targets EBP- (Emopamil-binding protein; D8-D7 sterol isomerase) dependent cholesterol biosynthesis and selectively induces cellular cholesterol depletion and apoptotic death in human colorectal cancer (CRC) cultures harboring APC truncations under lipid-deficient conditions (0.2% FCS or 2% lipoprotein-deficient serum; IC50 from 35 nM/HT29 to 4.9 μM/HT55 in 72 hrs) as a result of defective cholesterol homeostasis regulation, while exhibiting little cytotoxicity toward wild-type APC CRC cells or non-transformed human colonic and bronchial epithelial cells (IC50 >50 μM in 72 hrs). TASIN-1 intraperitoneal injection is efficacious against the growth of CRC tumors with trunctated APC using the genetically engineered CPC;Apc mice (20 mg/kg twice a week) and two xenograft murine models (DLD1 & HT29; 40 mg/kg twice daily) without apparent toxicity to the animals.
SML2260   Taspoglutide trifluoroacetate salt ≥95% (HPLC) Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist. Taspoglutide improves glucose tolerance, postprandial glucose, body weight, glycaemic control and insulin sensitivity in the Zucker diabetic fatty rat.
SML2489 Tasquinimod ≥98% (HPLC) Tasquinimod is an antineoplastic agent with immunomodulatory, anti-angiogenic and anti-metastatic activity. It showed good results in overall survival improvement in castrate resistant prostate cancer. Its mechanism of action is not known, but may involve Protein S100-A9 also known as migration inhibitory factor-related protein 14 (MRP-14).
SML2319   TAT-Gap19 trifluoroacetate salt ≥95% (HPLC) TAT-Gap19 is a cell penetrant analog of a connexin 43 (Cx43) hemichannels selective blocker Gap19. TAT-Gap19 inhibits TAT-Gap19 in mice brain without affecting gap junction channels.
T7329 Taurolidine >97% (NMR), powder Taurolidine is a broad spectrum antibiotic with antineoplastic activity, which induces apoptosis and decreases tumor cell proliferation. Taurolidine has been used with TNF-related-apoptosis-inducing ligand (TRAIL) to characterize synergistic responses in many apoptosis related signaling-proteins. Tauroline is also being used as a tool to study the various mechanisms of apoptosis and necrosis.
Taurolidine is an antibacterial agent that can be used for the treatment of peritonis. It has also been used as an antiendoxic substance for systematic inflammatory response syndrome and as an anti-angiogenic agent for tumors. Furthermore, studies have reported that taurolidine can be used for the prevention of multiple catheter-related bloodstream infections.
SML1227   Tavaborole ≥95% (HPLC) Tavaborole (AN2690) is a potent antifungal that targets the post-transfer editing site of leucyl-tRNA synthetase (LeuRS). Tavaborole forms a covalent adduct with the 3′ adenosine of tRNA(leu) at the editing site of fungal, but not bacterial LeuRS, locking the enzyme in an inactive conformation. Tavaborole was recently approved for the treatment of onychomycosis of the toenail in adults.
T7080   Tazarotene ≥98% (HPLC) Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. It is a prodrug of tazarotenic acid, which specifically activates RARb and RARg, only weakly activates RARa, and is inactive at retinoid X receptors (RXRs). In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.
SML1619 Tazarotenic acid ≥98% (HPLC) Tazarotene is transformed to tazarotenic acid with the help of esterases. Tazarotenic acid regulates the pathogenic aspects of psoriasis through normalizing abnormal keratinocyte differentiation. It possesses strong anti-hyperproliferative effects in skin and reduces inflammation.
Tazarotenic acid, an active metabolite of tazarotene, is a potent and selective agonist of the retinoid receptor (RAR) that binds to RARα, RARβ, and RARγ. Tazarotenic acid relatively selective activates RARβ and RARγ. Tazarotenic acid is a first xenobiotic substrate of human retinoic acid hydroxylase CYP26A1 and CYP26B1.
SML2144 TB5 ≥98% (HPLC) TB5 is a potent and selective reversible inhibitor of monoamine oxidase B (MAOB) with a Ki value of 110 nM. A reversible inhibitor should have an advantage over irreversible inhibitors such as selegiline in limiting side effects. Parallel artificial membrane permeation (PAMPA) assays indicated TB5 should be able to cross the blood–brain barrier. TB5 was found nontoxic to cells.
T0826 TBB ≥98% (HPLC), solid TBB binds to the Val66 residue of casein kinase-2 and inhibits the binding of ATP/GTP. TBB is cell permeable; it induces caspase-dependent apoptosis and degrades hematopoietic lineage cell-specific protein 1 in Jurkat cells.
TBB is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2) (IC50 = 900 nM and 1.6 mM, using rat liver and recombinant human CK2, respectively).
T6951 TBBz ≥98% (HPLC), powder TBBz is a cell-permeable Casein Kinase-2 (CK2) inhibitor. CK2 inhibitors, 4,5,6,7-tetrabromobenzotriazole (TBBt, Sigma Cat. # T0826) and rabromobenzimidazole (TBBz), the latter of which was shown to discriminate between different molecular forms of CK2 in yeast. TBBt, with a pK(a) ~5, exists in solution at physiological pH almost exclusively (>99%) as the monoanion; whereas TBBz, with a pKa ~9, is predominantly (>95%) in the neutral form, both of obvious relevance to their modes of binding. In vitro, TBBt inhibits different forms of CK2 with Ki values ranging from 80 to 210 nM. TBBz discriminates better between CK2 forms, with Ki values ranging from 70-510 nM. TBBz is more effective than TBBt in inducing apoptosis and to a lesser degree, necrosis in transformed human cell lines. Dvelopment of shRNA strategies for the selective knockdown of the CK2α and CK2α′ isoforms reinforces the foregoing results, indicating that inhibition of CK2 leads to attenuation of proliferation.
SML0854   TBCA ≥98% (HPLC) Tetrabromocinnamic acid (TBCA) is a selective cell-permeable ATP-competitive casein kinase CK2 inhibitor with an IC50 of 110 nM, 2-fold selectivity over CK1, and with the advantage of being less active on DYRK1A (IC50 = 24.5 μM) than other CK2 inhibitors suh as DMAT. Elevated levels of CK2 are associated with many cancers and also with tau hyperphosphorylation and neuropathology found in Alzheimer′s disease and other neurodegenerative disorders. In prostate cancer cells TBCA reduced cell proliferation and caused G2/M cell cycle arrest. In isolated squid axoplasms, TBCA also blocked inhibition of fast axonal transport by Aβ oligomers.
SML0453 TBPB ≥98% (HPLC) TBPB is a highly selective Muscarinic M1 receptor allosteric agonist. It activates M1 through an allosteric site rather than the orthosteric acetylcholine binding site, which is likely critical for its selectivity. Muscarinic 1 (M1) receptors are expressed in brain regions responsible for attention and memory, including hippocampus, cortex, and striatum. M1 activation is a proposed mechanism for increasing information processing in disease states, such as Alzheimer′s. M1 agonists are being studied as potential therapeutic agents to treat Alzheimer’s disease and the cognitive and negative symptoms of schizophrenia.
SML2789 tBPC ≥98% (HPLC) tBPC is a postitive allosteric modulator of the neuropeptide Y (NPY) Y4 receptor, which is predominantly expressed in the gastrointestinal tract and activated most strongly by pancreatic polypeptide (PP). tBPC was shown to potentiate Y4R activity in G-Protein signaling and arrestin3 recruitment and to potentiate the native PP response. tBPC was selective for Y4R over other Neuropeptide Y receptors and showed no effect on the efficacy (Emax) or potency (EC50) of the NPY signal response at the Y1, Y2, or Y5 receptors at 30 μM.
SML1299   TC-2153 ≥95% (HPLC) TC-2153 is a potent inhibitor of STEP (STriatal-Enriched protein tyrosine Phosphatase) that forms a reversible covalent bond with the catalytic cysteine in STEP. TC-2153 increases tyrosine phosphorylation of STEP substrates ERK1/2, Pyk2, and GluN2B in cell cultures. TC-2153 improves cognitive function in transgenic AD mice.
SML0910   TC3.6 ≥98% (HPLC) TC3.6 is a PDE7 selective inhibitor (IC50 = 1.04 μM). In an Experimental Autoimmune Encephalomyelitis (EAE) murine model, TC3.6 reduced levels of IL-17, blocked infiltration of immune cells into the CNS and elevated levels of the Treg marker Foxp3. TC3.6 also enhances survival and differentiation of oligodendrocyte precursor cells.
SML2446 TC-A2317 hydrochloride ≥98% (HPLC) Orally active, potent and selective aurora A kinase inhibitor with anti-cancer activity in vitro and in vivo.
TC-A2317 (TC-A 2317) is an orally active, potent and selective aurora A kinase inhibitor (Ki = 1.2 nM; Aurora B Ki = 101 nM; IC50 >1 μM toward 60 other kinases). TC-A2317 inhibits the proliferation of human colorectal carcinoma HCT116 cells in cultures (IC50 = 115 nM) and suppresses HCT116 xenograft-derived tumor growth in mice in vivo (by 59% on day 14; 30 mg/kg/day p.o.) with good pharmacokinectic properties, oral bioavailability (Tmax = 1.2 h, T1/2 = 3.3 h, Cmax = 4930 nM, C60 min = 52 nM in rat serum post 30 mg/kg p.o.), and no adverse effects to the animals. TC-A231 is a racemate with its (S)-enantiomer being more active than the (R)-enantiomer (respective Ki = 0.59 vs. 66 nM).
SML1402 TCID ≥98% (HPLC) TCID is a cell penetrant potent and specific inhibitor of UCH-L3 (Ubiquitin carboxyl-terminal hydrolase isozyme L3). TCID is used to distinguish between UCH-L1 and UCH-L3 activities in cells.
SML0416 TCN-201 ≥98% (HPLC) TCN-201 is a sulphonamide derivative, that negatively modulates glycine binding to the GluN1 (glutamate receptor subunit) subunit of the receptor.
TCN-201 is the first NMDA receptor antagonist that is specific for NR2A-subunit containing receptors. The pIC50 for NR2A NMDA receptors is 6.8. TCN-201has no effect on NR2B-containing receptors at concentrations up to 50 mM.
T1443 TCPOBOP ≥98% (HPLC), solid TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR. The most potent known member of the phenobarbital-like class of CYP-inducing agents.
human ... NR1I3(9970)
SML2117 TCS-1102 ≥98% (HPLC) TCS-1102 (DORA-1) is a high-affinity (Ki = 3 nM against [3H]-TCS-1102 for binding hOX1R and Ki = 0.2 nM against [3H]-pyrrolylphenyl analog for binding hOX2R) dual orexin receptor antagonist (DORA) that potently inhibits calcium mobilization in hOX1R & hOX2R CHO transfectants (IC50 = 17 & 4 nM, respectively). TCS-1102 promotes sleep (50-100 mg/kg p.o.), decreases fear/anxiety (10-20 mg/kg i.p.), and inhibits ADL-orexin B peptide-induced locomotion (by 56%/74%/100% with 15/50/100 mg/kg i.p. 30 min before ADL-XB ICV injection) with good pharmacokinetic properties, brain penetration (Brain/plasma conc. = 2.37 μM/3.50 μM 3 hrs post 100 mg/kg i.p.), and oral availability (Cmax/AUC(0–24h) = 1.21 μM/6.8 μM h and 3.01 μM/12.5 μM h, respectively post 50 and 100 mg/kg p.o. dosage) in rats in vivo.
SML2140 TCS 401 ≥98% (HPLC) TCS 401 is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B), which plays a key role in the negative regulation of the insulin signaling pathway, contributing to insulin resistance. It exhibited Ki values of 290 nM for PTP1B, with greater than 100-fold or more selectivity compared to other phosphatases. Inhibition of PTP1B by TCS 401 has been shown to sensitize the insulin signaling pathway and increase dopamine release in response to insulin. TCS-401 has also been shown to promote endothelial cell motility and to induce differentiation of retinal pigment epithelial cells toward improved contractility and motility.
SML2145 TD52 ≥98% (HPLC) TD52, an erlotinib analog, is a putative inhibitor of CIP2A that exhibits potent antitumor efficacy on HCC and TNBC cells. TD52 induces apoptosis through downregulation of CIP2A (Cancerous inhibitor of protein phosphatase 2A) in HCC, NSCLC and TNBC cells. Apparently TD52 indirectly downregulates CIP2A transcripts through interrupting the binding of Elk1 to CIP2A promoter. TD52 is a weak inhibitor of EGFR tyrosine kinase.
SML1539   TDFA trifluoroacetate salt ≥98% (HPLC) TDFA (Thr-Asp-F-amidine) is a selective inhibitor of peptidyl arginine deiminase 4 (protein arginine deiminase 4, PAD4 or PADI4), a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline, a process called citrullination. PAD4 is upregulated in cancer and inflammatory diseases, and may be involved in rheumatoid arthritis onset and progression. It has recently been found to be involved in the regulation of pluripotency: important for stem-cell gene activation, induced pluripotent stem (iPS) cell reprogramming, and maintenance of pluripotent cells in the early mouse embryo. TDFA has an IC50 value of 2.3 μM and is ≥15-fold selective for PAD4 versus PAD1 and ≥50-fold selective versus PADs 2 and 3.
T8325 TDZD-8 ≥98% (HPLC), needles TDZD-8 is a selective inhibitor of GSK-3, a thiadiazolidinone derivative, non-ATP competitive inhibitor of GSK-3β (IC50 = 2 μM). It does not inhibit Cdk-1/cyclin B, CK-II, PKA or PKC at >100 μM. TDZD-8 has been proposed to bind to the kinase site of GSK-3β.
SML2803 Tebanicline hydrochloride ≥98% (HPLC) New Tebanicline (ABT-594) is a partial agonist at neural nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. It is a less toxic analog of epibatidine with potent antinociceptive effects.
SML2846 Tebipenem pivoxil ≥98% (HPLC) New Tebipenem pivoxil (L-084I; ME1211; SPR994; Tebi-pivoxil; TBM-PI) corresponds to the orally bioavailable pivalyl ester prodrug form of the carbapenem class broad-spectrum β-lactam antibiotic Tebipenem (LJC 11,036; SPR859; TBM). TBM is potent against both gram-positive and gram-negative bacteria, including penicillin-resistant S. pneumoniae (PRSP) and many β-lactamase-producing strains, while being less effective against methicillin-resistant S. aureus (MRSA), S. marcescens, and P. aeruginosa. TBM is 2- to 64-fold more potent than imipenem, cefdinir, and faropenem against clinical isolates from respiratory and urinary-tract infections.
T7205 Tegafur ≥98% (HPLC), powder Tegafur is a pro-drug of 5-fluorouracil, an antimetabolite used as an antineoplastic agent. It has been used as adjuvant chemotherapy for curatively resected colorectal cancer therapy.
SML1504 Tegaserod maleate ≥98% (HPLC) It stimulates neurotransmitter release from enteric nerves and regularizes gastrointestinal function. Tegaserod has been used to treat irritable bowel syndrome associated with constipation and chronic constipation.
Tegaserod is a potent full agonist at serotonin 5-HT4 receptors with an EC50 of 7 nM.
human ... HTR4(3360)
T7330 Teijin compound 1 hydrochloride ≥98% (HPLC), powder Teijin compound 1 is CCR2b receptor antagonist. Teijin compound 1 inhibits cell chemotaxis induced by MCP-1. The chemokine receptors CCR2 is G protein-coupled receptors (GPCR), and is mainly expressed in monocytes, immature dendritic cells, activated T-lymphocytes and basophils.
SML0293 Telbivudine ≥98% (HPLC) Telbivudine is a nucleoside analog that is widely used to treat hepatitis B virus (HBV) infection.
T122 Telenzepine dihydrochloride hydrate solid, ≥98% (HPLC) Telenzepine is an analog of pirenzepine and inhibits the secretion of gastric acid. It is an antagonist to M1-receptor and targets the oxyntic gastric glands and the salivary glands.
human ... CHRM1(1128)
SML2162 Telithromycin ≥90% (HPLC) Telithromycin is a ketolide antibiotic, the first to enter clinical use. It is used to treat mild to moderate respiratory infections. Telithromycin binds to the subunit 50S of the bacterial ribosome, interfering with bacterial protein synthesis.
T8949 Telmisartan ≥98% (HPLC), solid Telmisartan is a non-peptide AT1 angiotensin receptor antagonist.
human ... AGTR1(185)
SML1707   Temoporfin ≥90% (HPLC) Temoporfin is a photosensitizer for the photodynamic therapy. Temoporfin has been used clinically to treat advanced head and neck squamous cell carcinoma, and is being investigated for use in several other cancers.
T2577 Temozolomide ≥98% (HPLC) Temozolomide is a DNA methylating agent and drug resistance-modifying agent; anti-tumor and anti-angiogenic. Temozolomide induces G2/M arrest and apoptosis through adduction of a methyl group to O6 position of guanine in genomic DNA and functional inactivation of DNA repair protein O(6)-alkylguanine DNA alkyltransferase (AGT) in base excision repair (BER) pathway.
PZ0020 Temsirolimus ≥98% (HPLC) Temsirolimus is a specific inhibitor of mammalian target of rapamycin (mTOR) mTOR Complex 1 (mTORC1). Temsirolimus is an antiproliferative and antiangiogenic, the first-in-class mTOR inhibitor approved for the treatment of patients with advanced poor prognosis renal cell carcinoma.
The inhibitory action of temsirolimus is mediated by FKBP-12 (FK506-binding protein 12), a major intracellular protein. It is useful in treating renal-cell carcinoma.
human ... FKBP1A(2280)
SML1441 Tenatoprazole ≥98% (HPLC) Tenatoprazole is a proton pump inhibitor. Tenatoprazole is an acid-activated prodrug that binds covalently to gastric H,K-ATPase, resulting in acid secretion inhibition. Tenatoprazole has a different structural class from omeprazole and most other proton pump inhibitors, with an imidazopyridine backbone rather than benzimidazole, which results in slower metabolism. Tenatoprazole thus has a long plasma half-life as compared to omeprazole, resulting in prolonged inhibition of acid secretion.
Tenatoprazole is used to maintain high diurnal and nocturnal pH levels. It prevents gastric H+,K+-ATPase with potency similar to omeprazole.
PZ0196   Tenidap ≥97% (HPLC) Tenidap is an anti-inflammatory and anti-rheumatic with a variety of activities. Tenidap preferentially inhibits COX-1 with an IC50 value of 30 nM, and also has some lesser inhibitory activity towards COX-2 and 5-lipoxygenase (IC50 values are 1.2 and > 30 μM for COX-2 and 5-lipoxygenase respectively). Tenidap is also a cytokine modulator, an opener of inward rectifying hKIR2.3 channels (EC50 = 402 nM) and has been shown to modulate cytoplasmic pH and inhibit anion transport in vitro.
SML0609   Teniposide ≥97% (HPLC) Teniposide (VM-26) is a Topoisomerase II inhibitor with antitumor activity. Teniposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA, inducing breaks in double stranded DNA and preventing repair.
SML1795 Tenofovir ≥98% (HPLC) Tenofovir has a low oral bioavailability. Hence, it is available as a prodrug called tenofovir disoproxil fumarate. Once ingested, tenofovir disoproxil fumarate is hydrolyzed to tenofovir and phosphorylated. This is then incorporated into the viral DNA which leads to chain termination. Tenofovir is also effective against hepatitis B virus.
Tenofovir is a nucleotide analogue reverse transcriptase inhibitor (nRTI) that causes premature termination of DNA transcription. Tenofovir is an antiretroviral used for HIV treatment and prevention.
SML1794 Tenofovir disoproxil fumarate ≥98% (HPLC) Tenofovir disoproxil fumarate (tenofovir DF) is a nucleotide analogue with activity against retroviruses, such as human immunodeficiency virus (HIV)-1, HIV-2 and hepadnaviruses.
Tenofovir disoproxil fumarate is a prodrug of tenofovir, a nucleotide analogue reverse transcriptase inhibitor (nRTI) that causes premature termination of DNA transcription. In a T cell line and primary blood lymphocytes, the antiviral activity of tenofovir disoproxil was shown to be more than 100-fold greater than tenofovir because of its rapid intracellular uptake. Tenofovir disoproxil fumarate has been used alone and in various combinations for the prevention and treatment of HIV/AIDS and chronic hepatitis B infections and is on the World Health Organization′s List of Essential Medicines.
Tenofovir disoproxil fumarate is a prodrug of tenofovir, a nucleotide analogue reverse transcriptase inhibitor (nRTI); anti-retroviral.
T3455 Terameprocol ≥98% (HPLC) Terameprocol is a synthetic derivative of NDGA, a non-selective lipoxygenase inhibitor. It inhibits Sp1 transcription factor binding at the HIV long terminal repeat promoter and at the α-ICP4 promoter, a gene essential for HSV replication, with IC50 values of 11 and 43.5 μM respectively. TMNDGA induces growth arrest and apoptosis by suppressing Sp1-dependent Cdc2 and survivin gene expression giving rise to its antitumorigenic activity. The in vivo growth of xenografts in numerous human tumor types was suppressed upon treatment with TMNDGA It also inhibits the growth of murine and human melanomas and human colon cancer in vivo without causing other tissue toxicity.
Terameprocol is known to reduce angiogenesis1.
T4680 Terazosin hydrochloride ≥98% (TLC), powder α1-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
T2528 Terbutaline hemisulfate salt Terbutaline is a β-adrenoceptor agonist and is known to function as a bronchodilator. Studies have reported that terbutaline is potent inhibitor of premature labor6.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
T9652 Terfenadine Non-sedating second generation H1 histamine receptor antagonist. Mainly metabolized by Cyp3A4, 5, 7. Inhibits CYP2C8.
Terfenadine acts a potential anti-histamine and is used in the treatment of allergic rhinitis and chronic urticaria.
human ... ABCB1(5243), CYP2C8(1558), CYP3A4(1576), HRH1(3269), IL4(3565), IL5(3567), KCNH1(3756), KCNH2(3757)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Hrh1(24448)
UC206   Terfenadine alcohol metabolite CYP3A4 metabolitye of terfenadine
SML0936   Teriflunomide ≥98% (HPLC) Teriflunomide is an orally available anti-inflammatory immunomodulator. It blocks the activity of dihydroorotate dehydrogenase, preventing pyrimidine synthesis and T and B cell proliferation and function. Teriflunomide has been used to treat rheumatoid arthritis and was recently approved for multiple sclerosis.
SML2424   Terlipressin acetate salt ≥98% (HPLC) Terlipressin is a synthetic vasopressin analog and agonist. It has been used as a vasoactive drug for treatment of Hepatorenal syndrome in cirrhosis of the liver.
T4577 Terodiline hydrochloride ≥98% (HPLC), solid Terodiline hydrochloride is a non-selective calcium channel antagonist with anticholinergic and vasodilatory activity.
Terodiline is known to increase corrected QT interval (QTc) and decrease resting heart rate in elderly patients. Furthermore, terodiline hydrochloride has been linked to cardiac arrhythmias1.
human ... CACNA1A(773), CACNA1B(774), CACNA1C(775), CACNA1D(776), CACNA1E(777), CACNA1F(778), CACNA1G(8913), CACNA1H(8912), CACNA1I(8911), CACNA1S(779), CACNA2D1(781), CACNA2D2(9254), CACNA2D3(55799), CACNA2D4(93589), CACNB1(782), CACNB2(783), CACNB3(784), CACNB4(785), CACNG1(786), CACNG2(10369), CACNG3(10368), CACNG4(27092), CACNG5(27091), CACNG6(59285), CACNG7(59284), CACNG8(59283), CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
SML1127   Terpendole E ≥95% (HPLC) Terpendole E is a mitotic kinesin Eg5 (Kinesin-5) inhibitor isolated from Albophoma yamanashiensis that inhibits both motor and microtubule stimulated ATPase activities of human Eg5. Studies indicate that Terpendole E inhibits Eg5 mutants resistant to S-trityl-L-cysteine and other Eg5 inhibitors. Also, Terpendole E is an ACAT (Acyl-CoA:cholesterol acyltransferase) inhibitor.
SML0480   Terreic Acid from Aspergillus terreus, ≥98% (HPLC) Terreic acid (TA) is a covalent inhibitor of the bacterial cell wall biosynthetic enzyme MurA. The survival of most bacteria depends on the functionality of this cytosolic enzyme. The inactivation of MurA requires the presence of UDP-N-acetylglucosamine 1-Carboxyvinyl transferase, which catalyzes the first step in the biosynthesis of the bacterial cell wall. TA is more potent than the known MurA inhibitor Fosphomycin. TA was also found to severely inhibit the transcription of TNFα and IL-2. TA inhibits protein synthesis by blocking the formation of leucyl-tRNA in sensitive bacteria and inhibits the catalytic effect of Bruton′s tyrosine kinase (Btk), an important factor in B-cell and mast cell activation, by inducing conformational changes that prevent Protein Kinase C (PKC) from interacting with the Btk domain. Moreover, recent studies have demonstrated that TA exhibits a very high level of radical scavenging activity.
T5705   Terrein from Aspergillus terreus, ≥98% (HPLC) Terrein is a bioactive fungal metabolite that has plant growth inhibition and antibacterial activities. Terrein reduces melanin levels in a dose-dependent manner as well as tyrosinase protein production. In mammals, there are three melanocyte-specific enzymes: tyrosinase, tyrosinase-related protein-1 (TRP-1), and TRP-2 that are involved in tyrosine conversion into melanin (melanogenesis). Terrein inhibits melanin synthesis by reducing tyrosinase production via extracellular signal-regulated protein kinase (ERK) activation. ERK activation is followed by microphthalmia-associated transcription factor (MITF) down regulation, which is required for tyrosinase expression.
SML1198 Terutroban ≥95% (HPLC) Terutroban is a highly selective and long-acting thromboxane/prostaglandin endoperoxide receptor (TPr) antagonist. The compound Terutroban blocks thromboxane induced platelet aggregation and vasoconstriction. Terutroban prevents vascular wall proliferation and atherogenesis, increases anti-oxidant enzymes like glutathione peroxidase, and has anti-inflammatory properties.
SML1369 Tesaglitazar ≥98% (HPLC) Tesaglitazar is a potent and specific dual PPARα/γ agonist that improves insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats.
human ... PPARA(5465), PPARG(5468)
T1500 Testosterone ≥98% Testosterone secreted by the testis is converted to dihydrotestosterone in the target tissues where it appears to mediate many of the biological actions of testosterone. Androgens direct the development of the male phenotype during embryogenesis and at puberty.
human ... AR(367), EBP(10682), ESR1(2099), PGR(5241), SERPINA6(866), SHBG(6462)
mouse ... Esr1(13982)
rat ... Ar(24208), Esr1(24890), Nr3c1(24413), Nr3c2(25672), Pgr(25154)
T8390 Testosterone 3-(O-carboxymethyl)oxime Androgens direct the development of male reproductive system and secondary sexual characteristics. Testosterone is an androgen that is secreted by the testis. This hormone is converted to dihydrotestosterone (DHT) by 5α reductase in the target tissues. Both DHT and testosterone require androgen receptor, a ligand-dependent nuclear transcription factor to mediate their biological functions.
Androgens direct the development of the male phenotype during embryogenesis and at puberty. Testosterone is an androgen that is secreted by the testis. This hormone is converted to dihydrotestosterone in the target tissues where it may mediate several biological functions.
T5771   Testosterone 3-(O-carboxymethyl)oxime: BSA - fluorescein isothiocyanate conjugate Studies have reported that BSA-coupled testosterone can block the growth of LNCaP cells. Furthermore, it can activate Fas protein and cell death, as well as reduce the translocation, adhesion and incursion of iAR-negative, DU145 prostate cancer cells2.
T1875 Testosterone propionate solid Androgens direct the development of the male phenotype during embryogenesis and at puberty. Testosterone is an androgen that is secreted by the testis. This hormone is converted to dihydrotestosterone in the target tissues where it regulates several biological functions. Testosterone propionate has been synthetically derived from a plant. This product has extended and faster-acting functions when compared to other testosterone esters.
human ... AR(367), CYP17A1(1586)
rat ... Ar(24208)
T3194   Tetanus toxin from Clostridium tetani Binds to polysialogangliosides acceptors on surface of all peripheral presynaptic nerve terminals. Internalized by receptor-mediated endocytosis and carried to spinal cord and brain by transsynaptic retrograde transport. Blocks the release of glycine from inhibitory interneurons of the spinal cord. Cleaves synaptobrevin (VAMP-2), and blocks synaptic vesicle exocytosis in vivo.
Tetanus toxin can cause spastic paralysis.
Clostridium tetani E88 ... tetX(1061100)
T3694   Tetanus toxin C fragment from Clostridium tetani Tetanus toxin is a neurotoxin that comprises of a heavy and a light chain linked by disulfide bridges. This neurotoxin enters the cytoplasm and releases the light chain component that subsequently inhibits the release of neurotransmitters2. Studies have reported that the fragment C of tetanus toxin retains most of the determinants that interact with thyroid membranes, gangliosides and neural membranes3.
T2952 Tetrabenazine ≥98% (HPLC), solid Tetrabenazine is a reversible type 2 vesicular monoamine transporter (VMAT) inhibitor. It depletes dopamine stores.
T7508 Tetracaine hydrochloride ≥99% Blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
T1698 Tetradecylthioacetic acid ≥97% (NMR) PPARα agonist; activation in ranking order: PPARδ > PPARα > PPARγ
Tetradecylthioacetic acid (TTA) is known to modulate lipid homeostasis. TTA can increase fatty acid oxidation and ketogenesis, which can subsequently prevent adiposity and insulin resistance. Furthermore, TTA can enhance cardiac functions during experimental heart failure.
human ... PPARA(5465)
T4425 (6R)-5,6,7,8-Tetrahydrobiopterin dihydrochloride Lack of tetrahydrobiopterin may cause hyperphenylalaninemia. Diseases like, Parkinson′s, autism, depression and Alzheimer′s shows low concentration of tetrahydrobiopterin in the cerebrospinal fluid. This coenzyme participates in dopamine (DA) synthesis.
human ... PAH(5053)
T2386 Δ9-Tetrahydrocannabinol solution ethanol solution Δ9-Tetrahydrocannabinol or Δ9-THC is a psychoactive ingredient in marijuana that is known to function as a neuroprotective antioxidant21. In vivo microdialysis studies have reported that Δ9-THC can enhance extracellular dopamine efflux in the nucleus accumbens of conscious, freely-moving rats22.
Agonist at CB1 and CB2 cannabinoid receptors. Hallucinogen; major psychoactive component of marijuana from Cannabis sativa.
human ... CNR1(1268), CNR2(1269)
mouse ... Cnr1(12801)
rat ... Cnr1(25248)
T200 (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate ≥97% (HPLC), solid TPMPA is a hybrid of isoguvacine and 3-APMPA designed to retain affinity for GABAC receptors but not to interact with GABAA or GABAB receptors. Electrical assays show that TPMPA is a competitive antagonist of cloned human mu 1 GABAC receptors expressed in Xenopus laevis oocytes (Kb approx. 2 μM). TPMPA is >100-fold weaker as an inhibitor of rat brain GABAA receptors expressed in oocytes (Kb approx. 320 μM) and has only weak agonist activity on GABAB receptors assayed in rat hippocampal slices (EC50 approx. 500 μM). TPMPA may be used to investigate GABAC receptor function in the outer retina and in any other areas of the nervous system in which these types of receptor are present.
SML0834 2,3,5,4′-Tetrahydroxystilbene 2-O-β-D-glucoside ≥98% (HPLC) 2,3,5,4′-Tetrahydroxystilbene 2-O-β-D-glucoside induces the expression and enhances the activity of EPO. The compound stimulates mitochondrial biogenesis, and expression of hemoglobin in non-hematopoietic cells. 2,3,5,4′-Tetrahydroxystilbene 2-O-β-D-glucoside has demonstrated protective effects in cardiovascular disease and ischemia models.
2,3,5,4′-Tetrahydroxystilbene 2-O-β-D-glucoside (THSG) elicits anti-inflammatory, antioxidative and anti-atherosclerotic functionality. It also provides protection against cytotoxicity in neuroblastoma cells induced by 1-methyl-4-phenyl pyridium (MPP+) as well as MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) induced Parkinson′s disease. By its antioxidative functionality, it blocks lipid peroxidation in Alzheimer′s disease model. In ligature-induced periodontitis, THSG inhibits inflammation.
T5955 3,4,5,6-Tetrahydroxyxanthone hydrate ≥98% (HPLC) 3,4,5,6-Tetrahydroxyxanthone is a Na/K-ATPase inihibitor that inhibits pump function without activating the kinase signaling function. It inhibits Na/K ATPase pump action with an affinity comparable to ouabain, but does not alter Na or ATP affinity, is not blocked by potassium, and it does not activate the Src complex or downstream kinases.
T4264 Tetrahydrozoline hydrochloride ≥98% (HPLC) α-adrenoceptor agonist; imidazoline binding site ligand; vasoconstrictor.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
T3787 3,3′,5,5′-Tetraiodothyroacetic acid 3,3′,5,5′-Tetraiodothyroacetic acid (Tetrac) is a deaminated analog of L-thyroxine (T4). It prevents the pro-angiogenesis actions of T4 and 3,5,3′-triiodo-L-thyronine. It is a thyrointegrin receptor antagonist. Tetrac prevents the binding of thyroid hormones.
Studies in rats have reported that Tetrac may regulate TSH secretion under in vivo conditions1.
P4413 N,N,N′,N′-Tetrakis(2-pyridylmethyl)ethylenediamine N,N,N′,N′-Tetrakis(2-pyridylmethyl)ethylenediamine (TPEN) elicits pro-apoptotic effect in human acute promyelocytic NB4 cells by inhibiting nitric oxide signalling and Zn2+ signaling. In microglia pretreated with zinc, TPEN inhibits the interleukin 6 secretion and nitric oxide synthase (iNOS) mRNA expression. It induces damage on DNA structure by activating ATM (ataxia telangiectasia mutated) and ATR (ATM-Rad3-related) signaling in human colon cancer cells.
TPEN is a membrane-permeable zinc chelator; decreased the intracellular level of zinc and induced apoptosis (i.e., cell shrinkage and formation of apoptotic bodies with DNA fragmentation and formation of a typical DNA ladder pattern).
SML0963   (E)-3,4,5,4′-Tetramethoxystilbene ≥98% (HPLC) (E)-3,4,5,4′-Tetramethoxystilbene (DMU 212) is a derivative of resveratrol with anti-angiogenic and anti-tumor properties.
SML1758 Tetrazanbigen ≥98% (HPLC) Tetrazanbigen (TNBG) is a potent and selective antitumor drug that induces lipid accumulation in cancer cells. Tetrazanbigen induces S phase arrest and apoptosis in hepatocellular carcinoma QGY-7701. Tetrazanbigen potently inhibits growth of QGY-7701 cells xenografts in mice.
SML1626 TFCA ≥98% (HPLC) TFCA is a Liver X receptor α (LXRα) antagonist that reduces lipid accumulation and fatty liver in mice. Apparently TFCA binds to the LXR? ligand binding domain and induces interaction with NCoR corepressor.
T7830 TFLLR-NH2 trifluoroacetate salt >98% (HPLC) TFLLR-NH2 is a protease-activated receptor (PARs) agonist which is more selective to PAR-1 than SFLLRN-NH2. Protease-activated receptors (PARs) are present on various organs including, plateles, mast cell, gallblader, oesophagus etc, and regulate various physiological processes including human platelet aggregation, vascular contraction/relaxation, and an increase in endothelial permeability. Recent papers indicated that PAR′s are also involved in sensory processing. Specificly PAR ligands enhance glutamatergic excitatory transmission in substantia gelatinosa (SG) neurons of adult rat spinal cord slices.
SML0342 TFM-4AS-1 ≥98% (HPLC) TFM-4AS-1 is a potent SARM (Selective Androgen Receptor Modulator). TFM-4AS-1 is a partial agonist of AR. The compound promotes the buildup of bone and muscle mass while having reduced effects on reproductive organs and sebaceous glands. The compound also is an inhibitor of rat 5 α-reductase enzymes type I (2 nM) and type 2 (3 nM).
SML2563 TFMB-(S)-2HG ≥98% (HPLC) TFMB-(S)-2HG is a membrane-permeant (S)-2-hydroxyglutarate (L-2HG) precursor used in conjunction with the oncometabolite (R)-2-hydroxyglutarate (D-2HG) precursor for probing 2-HG enantiomer-specific cellular responses (typical conc used in culture: 0.5-20 mM). While both 2HG enantiomers inhibit multiple α-ketoglutarate (α-KG; 2-OG)-dependent dioxygenases by competing against α-KG binding, (S)-2HG is reported to be more potent against TET1/2, CeKDM7A & KDM5B (JARID1B/PLU-1). On the other hand, (R)-2HG, but not (S)-2HG, is shown to downregulate HIF-1a by promoting EglN1 (HIF prolyl hydroxylase 2; HIF-PH2; PHD2) activity.
T5575 TG003 ≥98% (HPLC) Potent, specific, reversible, and ATP-competitive inhibitor of Cdc2-like kinase (Clk). Ki = 10 nM for mClk1/Sty; IC50 = 15 nM, 20 nM, 200 nM, and > 10 mM for mClk4, mClk1, mClk2, and mClk3, respectively.
TG003 regulates alternative splicing and reduces the phosphorylation of SF2/ASF1.
TG003, a CLK (cdc2-like kinase) family inhibitor is used as a drug for duchenne muscular dystrophy.
SML1217   TG4-155 ≥98% (HPLC) TG4-155 is a brain penetrant prostaglandin EP2 specific antagonist. TG4-155 has a 4730X selectivity over EP4 (2.4 nM vs 11.4 mM in binding assays), and a 7 fold selectivity over DP1 receptors. TG4-155 crosses the blood brain barrier, and has no antagonistic effects on EP4 signaling, and displays neuroprotective effects in a pilocarpine-induced status epilepticus (SE) seizure model. TG4-155 does not interfere with G-protein function or phosphodiesterase activity, and does not inhibit COX-1 or COX-2.
SML0136 TGN-020 ≥98% (HPLC) TGN-020 is an inhibitor of Aquaporin 4 (AQP4), the most abundant water channel in brain. Aquaporins (AQPs) are water channels required for maintaining fluid homeostasis and enabling water movement across barrier membranes, but can enhance pathological cellular volume changes and cause edema in injury states. Pretreatment with the AQP4 inhibitor TGN-020 significantly reduced the volume of brain edema associated with ischemic injury in a mouse model of focal cerebral ischemia.
SML1741 TH1020 ≥95% (HPLC) TH1020 is a non-cytotoxic non-cytotoxic toll-like receptor 5 (TLR5)/flagellin complex inhibitor. TH1020 selectively prevents flagellin-induced TLR5 signaling without affecting ligands-induced activation of TLR2, TLR3, TLR4, TLR7 or TLR8.
SML2275 TH-257 ≥98% (HPLC) TH-257 is a potent, type III allosteric LIM-kinase (LIMK1 & LIMK2) inhibitor (LIMK1/2 IC50 in nM = 48/29 by cell-free kinase assay and 250/150 by live cell NanoBRET assay using respective transfectants) that targets LIMK1/2 DFG-out conformation in a non-ATP-competitive manner and exhibits no significant off-target activity by KINOMEscan assay at 1 μM. TH-263 is a structure analog and the recommended negative control for TH-257. For characterization details of TH-257, please visit the TH-257 probe summary on the Structural Genomics Consortium (SGC) website.

TH-263 is the negative control for the active probe, TH-257. TH-263 is available from Sigma. To learn more about and purchase TH-263, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
SML1069 TH287 hydrochloride ≥98% (HPLC) TH287 is a potent inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with an IC50 value of 0.8 nM. MTH1 hydrolyzes oxidized purine nucleoside triphosphates that might otherwise be incorporated into DNA/RNA and contribute to DNA damage. MTH1 removal of oxidized nucleotides that result from increased levels of reactive oxygen species (ROS) in fast-proliferating cancer cells helps protect cancer cells from proliferative stress and prevent cancer cell death. TH287 is considered a new target for cancer therapy. TH287 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family. TH287 has been shown to selectively kill a variety of cancer cell lines, but is rapidly metablized, so not as useful for in vivo studies.
SML2531 TH5487 ≥98% (HPLC) TH5487 is an inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1), which is part of the DNA base excision repair pathway. TH5487 as shown to inhibit OGG1-dependent proinflammatory gene expression by binding in the OGG1 active site, preventing OGG1 from engaging damaged DNA in vitro and in cells, resulting in decreased proinflammatory gene expression.
SML1096 TH588 hydrochloride ≥98% (HPLC) TH588 is a potent inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with an IC50 value of 5 nM and good metabolic stability. MTH1 hydrolyzes oxidized purine nucleoside triphosphates that might otherwise be incorporated into DNA/RNA and contribute to DNA damage. MTH1 removal of oxidized nucleotides that result from increased levels of reactive oxygen species (ROS) in fast-proliferating cancer cells helps protect cancer cells from proliferative stress and prevent cancer cell death. TH588 is considered a new target for cancer therapy. TH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.
T150 (−)-Thalidomide >98%, solid (-)-Thalidomide selectively inhibits the biosynthesis of tumor necrosis factor α (TNF-α), which is essential for inflammatory response. It is an anti-emetic drug and is used to treat morning sickness in pregnant women. Thalidomide is also used to treat leprosy, multiple myeloma, Crohn′s disease and human immunodeficiency virus (HIV) infection. Thalidomide also inhibits angiogenesis. It is associated with several diseases such as, peripheral neuropathy, facial palsies, Duane syndrome and autism.
human ... LITAF(9516), TNF(7124)
mouse ... Nos2(18126)
rat ... Nos1(24598)
T151 (+)-Thalidomide ≥98% (HPLC), powder (-)-Thalidomide selectively inhibits biosynthesis of tumor necrosis factor α (TNF-α). (R)-Thalidomide is called "safe enantiomer", but it can be converted in the body to (S)-isomer.
human ... LITAF(9516), TNF(7124)
mouse ... Nos2(18126)
rat ... Nos1(24598)
T144 (±)-Thalidomide ≥98%, powder (±)-Thalidomide selectively inhibits biosynthesis of tumor necrosis factor α (TNF-α). It also functions as an inhibitor of angiogenesis, an immunosuppressive agent, a sedative and a teratogen. Furthermore, thalidomide is known to exhibit antitumor functions in refractory multiple myeloma.
human ... CRBN(51185), CUL4A(8451), DDB1(1642), LITAF(9516), RBX1(9978), TNF(7124)
mouse ... Nos2(18126)
rat ... Nos1(24598)
SML2686 THAL-SNS-032 ≥98% (HPLC) THAL-SNS-032 is a selective inhibitor and degrader of cyclin-dependent kinase 9 (CDK9). It links the CDK inhibitor SNS-032 to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon. THAL-SNS-032 was found to selectively induce degradation of CDK9 over other CDKs. It inhibited proliferation across a panel of 11 different leukemia cancer cell lines potently than SNS-032.
T9033 Thapsigargin ≥98% (HPLC), solid film Potent, cell-permeable, IP3-independent intracellular calcium releaser. Blocks the transient increase in intracellular Ca2+ induced by angiostatin and endostatin. Induces apoptosis by disrupting intracellular free Ca2+ levels; incorporated into chemotherapeutic prodrug formulations.
SML1845   Thapsigargin Ready Made Solution ≥98% (HPLC), 10 mM in DMSO Thapsigargin is an effective inhibitor of calcium ion pumps located on sarcoplasmic reticulum (SR) and endoplasmic reticulum (ER) microsomes of skeletal, cardiac, muscle and brain tissues.
Thapsigargin is an effective inhibitor of calcium ion pumps located on sarcoplasmic reticulum (SR) and endoplasmic reticulum (ER) microsomes of skeletal, cardiac, muscle and brain tissues. The inhibition of calcium ion pumps causes intracellular increase of calcium ion levels. It was found that thapsigargin at 100 nM concentration effectively inhibited the SR Ca2+- adenosine triphosphatase (ATPase) in cardiac and skeletal muscles. Thapsigargin was also reported to be effective in blocking autophagy by interfering with the autophagosome-lysosome fusion.
SML1456 Thaxtomin A ≥98% (HPLC) Cellulose synthesis inhibition by thaxtomin A, indicates plant-pathogen interaction. Along with this, it also results in hypocotyls swelling and decreased seedling growth. Thaxtomin A leads to common scab disease in potato. On the whole, it attenuates cell growth and induces cell death in the infected plant.
Thaxtomin A is a nitrated diketopiperazine phytotoxin produced by Streptomyces scabies that induces plant cells necrosis. Thaxtomin A is a potent plant cellulose synthesis inhibitor.
T2019 Thebaine powder The (-)-isomer of thebaine is the naturally-occurring constituent of opium that is a precursor of morphine. It has poor antinociceptive activity and induces convulsions. It binds to μ and δ opioid receptors in vitro.
T4500 Theobromine ≥98.0% Phosphosdiesterase inhibitor; weak adenosine receptor antagonist; diuretic; smooth muscle relaxant.
Theobromine possesses antitussive action and might be useful in treating acute and chronic cough. It is a catabolic product of caffeine and shows antioxidant and prooxidant properties.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora1(29290)
T1633 Theophylline anhydrous, ≥99%, powder Phosphodiesterase inhibitor; diuretic; cardiac stimulant; muscle relaxant; asthma medication.
Theophylline is a tea alkaloid that functions as a nonselective PDE4 inhibitor. It can induce smooth muscle relaxation in the bronchiolae of asthma patients. At increased concentrations, theophylline can function as a reprotoxic agent and can cause infertility by incapacitating Sertoli cells. This subsequently causes the premature release of late differentiating spermatogenic cells.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140), PDE3A(5139), PDE3B(5140), PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144)
mouse ... Adora2b(11541)
rat ... Adora1(29290), Adora2a(25369), Adora2b(29316), Pde1b(29691), Pde3a(50678)
T6330 THI 2-Acetyl-4-tetrahydroxybutyl imidazole (THI) is known to induce peripheral blood lymphopenia in rats. Studies in rats have also reported that THI can affect lymphocyte migration and degradation.
THI is an inhibitor of sphingosine-1-phosphate lyase and acts as an immunosuppressant. Sphingosine-1-phosphate (S1P) lyase catalyzes the irreversible decomposition of S1P to hexadecanaldehyde and phosphoethanolamine. Reducing S1P lyase activity results in therapeutic levels of immunosuppression without the non-lymphoid lesions that result from synthetic S1P receptor agonists.
SML0244 Thiamet G ≥98% (HPLC) Thiamet G is a potent inhibitor of the enzyme O-GlcNAcase (Ki = 21 nM). The compound is orally bioavailable and crosses the blood brain barrier. Thiamet G leads to an increase in O-GlcNAc-modified proteins in cell-based and in vivo assay systems, and reduces levels of phosphorylated Tau protein in rat cortex and hippocampus.
SML1045   Thiazovivin ≥98% (HPLC) Thiazovivin is a Rho Kinase (ROCK) inhibitor that promotes the transformation of fibroblasts into stem cells with a 200-fold efficiency over the classic method when used in combination with ALK5 inhibitor SB-431542 (S4317) and MEK inhibitor PD-0325901 (PZ0162). Thiazovivin stabilizes E-cadherin on the cell surface, necessary for human embryonic stem cell survival in culture. When human embryonic stem cells are cut out from the colony, this key protein is disrupted and then internalized within the cell. Without e-cadherin on the cell surface, cell signaling between the cells and their environment is disrupted and the cells quickly die.
Thiazovivin is an inhibitor of Rho associated coiled-coil containing protein kinase (ROCK). In vitro studies prove that thiazovivin is efficient in stimulating better morphology, expression of ionic transporter and protein involved in cell adhesion.
SML0954   Thiocolchicine ≥97% (HPLC) Thiocolchicine is an antimitotic alkaloid and apoptosis inducer that inhibits tubulin polymerization and microtubule assembly.
SML1476 Thiocolchicoside ≥98% (HPLC) Thiocolchicoside acts as a muscle relaxant. In experimental animals, thiocolchicoside results in malfunctions (teratogenic) and impairs chromosomes. It is advised to be used as an analgesic for patients with muscle pain, starting with paracetamol. Thiocolchicoside can be used in irrigation solution at the time of endoscopic treatment of ureteral calculus to reduce the movement of stones.
Thiocolchicoside is a potent competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist with muscle relaxant, anti-inflammatory, and analgesic activity. Thiocolchicoside has also been found to suppress nuclear factor kappa B ligand (RANKL) activation of NF-KB resulting in suppression of osteoclastogenesis.
SML1296 6-Thio-2′-Deoxyguanosine ≥97% (HPLC) 6-Thio-2′-deoxyguanosine (6-thio-dG) is a nucleoside analog and telomerase substrate that is incorporated into de novo–synthesized telomeres. 6-Thio-2′-deoxyguanosine induces telomere dysfunction and rapid cell death in cancer cells, while spearing telomerase-negative cells.
SML2310 Thiodigalactoside ≥98% (HPLC) Thiodigalactoside (TDG)is a potent inhibitor of galectin-1 (GAL1) that suppress tumor growth by inhibiting multiple cancer enhancing activities of galectin-1, including immune cell dysregulation, angiogenesis and protection against oxidative stress. Thiodigalactoside reverses galectin-1-induced cisplatin resistance in HCC cells. Thiodigalactoside significantly reduces body weight gain in diet-induced obese rats.
T3450 Thiolutin from Streptomyces luteosporeus, ≥95% (HPLC) Sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. It was found to inhibit in vitro RNA synthesis directed by all three yeast RNA polymerases (I, II, and III). Thiolutin is also an inhibitor of mannan and glucan formation in Saccharomyces cerevisiae and used for the analysis of mRNA stability. Studies have shown that thiolutin inhibits adhesion of human umbilical vein endothelial cells (HUVECs) to vitronectin and thus suppresses tumor cell-induced angiogenesis in vivo.
T1019 (±)-Thiopental Thiopental is an anesthetic that decreases cerebral metabolic rate without altering the blood flow or oxygen consumption.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
T123 Thioperamide maleate salt solid Potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier.
Thioperamide is a potent and selective H3 histamine receptor antagonist that crosses the blood-brain barrier. It affects the central histaminergic system and decreases the duration of seizures and convulsions in mice. It also improves learning deficit induced by other drugs such as scopolamine.
human ... HRH3(11255)
SML1120 Thiophene-2 ≥98% (HPLC) Thiophene-2 (TP2) is an inhibitor of polyketide synthase 13 (Pks13), which plays a critical role in the biosynthesis of mycolic acid, an essential component of the cell wall in M. tuberculosis, and is a potential new target for tuberculosis treatment. TP2 inhibits FadD32-dependent loading of the mycolic acid precursor meromycoloyl chain onto acyl carrier protein (ACP) domains located at the N terminus of Pks13, preventing synthesis of mycolic acid and resulting in mycobacterial cell death. TP2 bacteriosidal activity is equivalent to treatment with the first-line drug isoniazid, and enhances its activity, but is less likely to cause resistance. The minimal inhibitory concentration (MIC) values of TP2 against drug-susceptible multidrug-resistant M. tuberculosis strains is approximately 1 μM.
SML1151 Thiophene-4 ≥98% (HPLC) Thiophene-4 (TP4) is an inhibitor of polyketide synthase 13 (Pks13), which plays a critical role in the biosynthesis of mycolic acid, an essential component of the cell wall in M. tuberculosis, and is a potential new target for tuberculosis treatment. TP4 inhibits FadD32-dependent loading of the mycolic acid precursor meromycoloyl chain onto acyl carrier protein (ACP) domains located at the N terminus of Pks13, preventing synthesis of mycolic acid and resulting in mycobacterial cell death. TP4 bacteriosidal activity is equivalent to treatment with the first-line drug isoniazid, and enhances its activity, but is less likely to cause resistance. The minimal inhibitory concentration (MIC) values of TP4 against drug-susceptible multidrug-resistant M. tuberculosis strains is approximately 500 nM.
T9025 Thioridazine hydrochloride ≥99% D2 dopamine receptor antagonist; phenothazine antipsychotic with reduced extrapyramidal side effects; Ca2+ channel blocker.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2C(3358)
T6031 DL-Thiorphan ≥98% (TLC) Enkephalinase inhibitor.
human ... ACE(1636), ECE1(1889)
rat ... Ace(24310), Mme(24590)
T8902 Thiostrepton from Streptomyces azureus ≥90% (HPLC) Peptide antibiotic that prevents the binding of elongation factor G (EF-G) and GTP to the 50S ribosomal subunit.
SML2449 THIQ ≥98% (HPLC) THIQ is a selective tetrahydroisoquinoline melanocortin-4 receptor (MC4R) agonist. It exhibited an IC50 vaue of 1.2 nM in MC4R human receptors expressed in CHO cells compared values of 2067, 761 and 326 nM for MC1R, MC3R, and MC5R receptors, respectively.
SML1548 THPN ≥98% (HPLC) THPN is potent nuclear receptor TR3 (Nur77) antagonist that induces autophagic cell death in melanoma. Co-application of THPN with Akt2 inhibitors significantly represses tumor growth in xenograft mouse model.
SML0035 Tiagabine hydrochloride ≥98% (HPLC) Tiagabine hydrochloride is an anticonvulsant and selective GABA reuptake inhibitor through inhibition of the synaptic GABA transporter GAT1.
Tiagabine increases the synaptic GABA and enhances the neuronal inhibition. It is effective as adjunctive treatment of epilepsy and anxiety disorders.
human ... SLC6A1(6529)
T1692 Tianeptine sodium salt hydrate ≥98% (HPLC), powder Tianeptine is a tricyclic antidepressant that enhances serotonin uptake. This drug can affect neuroprotection, neuronal excitability, memory and anxiety. However, tianeptine is not linked to adverse psychomotor, cognitive, cardiovascular, sleep and bodyweight effects. The drug has a low tendency for abuse and has a positive pharmacokinetic profile.
Tianeptine is least involved in drug interaction as it is not metabolized by cytochrome P450 system in the liver. In hippocampus and amygdala, tianeptine is involved in glutamatergic transmission processes and elicits neuroplasticity.
SML0941   Tibolone ≥98% (HPLC) Tibolone is a selective tissue estrogenic activity regulator (STEAR) used for the treatment of the symptoms associated with menopause and also for the treatment of osteoporosis. Tibolone has estrogenic, progestogenic, and/or androgenic activity depending on the tissue. Three major metabolites of tibolone are responsible for its tissue selective mechanism of action. Conversion into 3α- and 3β-hydroxy-tibolone results in estrogenic effects in brain, vagina, and bone. The Δ4 isomer has progestrogenic and androgenic effects and does not cause estrogenic stimulation in the endometrium.
SML1068   TIC10 angular ≥98% (HPLC) TIC10 (TRAIL-inducing compound 10) induces apoptosis mediated by TRAIL (TNF-related apoptosis-inducing ligand) in a number of cancers without toxicity such as breast, colon and glioblastoma multiforme tumors.
TIC10 angular is a potent blood brain barrier penetrant and orally active inducer of TRAIL production that induces death of multiple human cancers. TIC10 angular inactivates both Akt and ERK, which results in Foxo3a nuclear factor migration to the nucleus and binding to TRAIL promoter.
SML2482 Ticagrelor ≥98% (HPLC) Ticagrelor is an antithrombotic antiplatelet drug that acts by direct and reversible competitive inhibition of the adensoine purinoceptor P2Y12 receptor.
human ... P2RY12(64805)
SML0339 Tideglusib ≥98% (HPLC) Tideglusib, also known as NP031112 or NP-12, is a potent non ATP-competitive inhibitor of glycogen synthase kinase-3 (GSK3), an important kinase studied in stem cell research and neurodegenerative diseases. It is currently in clinical trials for Alzheimer′s disease and Progressive Supranuclear Palsy (PSP). Tideglusib reduces phosphorylation of the tau protein and the accumulation of amyloid plaques, reduces hippocampal and entorhinal cortex neuron loss and improves spatial memory deficits. It has also shown neuroprotective and anti-inflammatory activity in a variety of animal models.
human ... GSK3B(2932)
SML0505 Tienilic Acid ≥98% (HPLC) Tienilic Acid (Ticrynafen) is a P450 inhibitor, a specific suicide substrate for CYP2C9 and CYP2C10. It was once used as a loop diuretic drug with uric acid-lowering (uricosuric) actvity, but was removed from market because of hepatotoxicity.
PZ0021 Tigecycline hydrate ≥98% (HPLC) Tigecycline is a broad spectrum glycylcycline antibiotic. Tigecycline is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline is active against resistant strains of gram-positive and gram-negative bacteria, avoiding the two most common mechanisms of resistance to the tetracycline antimicrobials: tetracycline efflux pump proteins and ribosomal protection proteins.
T4580 Tiludronate disodium salt hydrate ≥98% (HPLC) Tiludronate is a bisphosphonate bone resorption inhibitor. Tiludronate inhibits protein-tyrosine-phosphatase, leading to detachment of osteoclasts from the bone surface. It also inhibits the osteoclastic proton pump and is used to treat Paget′s disease.
T6454 Anti-Timeless (C-terminal) antibody produced in rabbit ~1.0 mg/mL, affinity isolated antibody, buffered aqueous solution Timeless (Tim) forms a complex with Tim interacting protein (Tipin), found by two-hybrid screening. It associates with components of the replication fork complex through direct binding with the (RPA) and are important for efficient DNA synthesis. Timeless plays a role in replication checkpoint responses to genotoxic stress. It also plays an important role in the maintenance of genome stability during unperturbed DNA replication. Overexpression of the TIMELESS gene is associated with cervical cancer. Annihilation of this gene induces apoptosis and cell senescence.
human ... TIMELESS(8914)
T6394 Timolol maleate salt ≥98% (TLC), powder Timolol maleate is a class II anti-arrhythmic agent that functions as a non-selective β-adrenoceptor antagonist, a vasodilator and an anti-glaucoma agent. Studies have reported that timolol maleate can be used for the treatment of infantile hemangioma (IH)7.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
SML2008 Tiotropium bromide monohydrate ≥98% (HPLC) Tiotropium Bromide is an anticholinergic broncholidator. It is considsered a long acting muscarinic receptor antagonist (LAMA) and is used clinically as an inhaled bronchodilator for COPD and asthma.
SML2369 Tipelukast ≥98% (HPLC) Tipelukast is a Leukotriene D4 (LTD4) receptor antagonist and an inhibitor of 5-lipoxygenase (5-LO) and also phosphodiesterases PDE3 and PDE4. It has been found to have antifibrotic and anti-inflammatory activity. Tipelukast has been investigated as a possible treatment for nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH).
SML1668 Tipifarnib ≥98% (HPLC) Tipifarnib (R115777) is an orally active and potent farnesyltransferase (FTase) inhibitor that exhibits potent anti-tumorigenic effects. Tipifarnib mechanism of action is not fully understand.
SML1552 Tipiracil hydrochloride ≥98% (HPLC) Tipiracil is an inhibitor of thymidine phosphorylase. Tipiracil is used in combination with trifluridine as TAS-102 for the treatment of refractory metastatic colorectal cancer. Tipiracil increases the bioavailability of trifluridine by blocking the enzyme that would otherwise protect the tumors by metabolizing trifluridine.
human ... TYMP(1890)
SML2312 Tipranavir ≥98% (HPLC) New Tipranavir is a HIV protease inhibitor that is highly potent against a variety of HIV strains and isolates in several cell culture systems. Tipranavir inhibits the replication of viruses that are resistant to other protease inhibitors.
T2825 TIQ-A ≥98% (HPLC), solid TIQ-A is a potent inhibitor of PARP, anti-apoptotic.
SML0552 Tirapazamine ≥98% (HPLC) Under hypoxic conditions, tirapazamine is a potent cytotoxic agent that induces apoptosis by inducing breaks in single and double stranded DNA, as well as chromosomal breaks. The compound sensitizes cells to other ionizing radiation and other cytotoxic agents like cisplatin.
SML0246 Tirofiban hydrochloride monohydrate ≥98% (HPLC) Tirofiban hydrochloride is a potent non-peptide, glycoprotein IIb/IIIa inhibitor. Blocks platelet aggregation and thrombus formation.
Tirofiban might cause thrombocytopenia.
human ... ITGA2B(3674), ITGB3(3690)
T6950 Tizanidine hydrochloride ≥98% (HPLC), powder α2-adrenoceptor agonist.
Tizanidine hydrochloride is known to function as a skeletal muscle relaxant that acts centrally. Furthermore, this relaxant functions at spinal and supraspinal levels to block excitatory interneurons. This drug is used for the symptomatic relief of spasticity and painful muscle spasms.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
SML2837 Tizoxanide ≥98% (HPLC) New Tizoxanide (TIZ) is the active metabolite of the broad-spectrum parasiticidal drug nitazoxanide (NTZ), a noncompetitive inhibitor against bacterial pyruvate-ferredoxin oxidoreductase (PFOR Ki 2 to 10 μM). NTZ deacetylates rapidly to TIZ in plasma (t1/2 ~6 min at 37°C in human plasma) and in the presence of liver microsomes. NTZ is also reported to exhibit antiviral activity against Hepatitis C, Norovirus, Paramyxovirus, Influenza, Vaccinia, and Zika.
SML0832   TLR4-IN-C34 ≥98% (HPLC) TLR4-IN-C34 is a potent and specific inhibitor of toll-like receptor 4 (TLR4), which inhibits TLR4 signaling in vivo and in vitro. TLR4-IN-C34, also known as C34, is an aminomonosaccharide that inhibits TLR4 signaling by docking with the hydrophobic pocket of the TLR4 co-receptor, myeloid differentiation protein-2 (MD-2). C34 has been shown to diminish the severity of experimental necrotizing enterocolitis (NEC).
T2955 γ6 TM1a trifluoroacetate salt ≥95% (HPLC) The calcium channel γ family is a subgroup of the tetraspanin proteins. There are the eight γ subunits that have been identified to date. Among these γ1 subunit acts as an endogenous antagonist of the skeletal HVA calcium current, and γ6 inhibits the low voltage-activated (LVA) Cav3.1 calcium current. A GxxxA motif in the first transmembrane domain (TM1) of γ6 was identified as critical for inhibiting the Cav3.1 current. γ6 TM1a is an octapeptide contains residues 41 through 48 of the native γ6 protein. The peptide inhibits the Cav3.1 calcium current in a dose-dependent manner. The reduction of channel current is mostly due to the inhibition of both resting and inactivated channels relatively independent of membrane potential. Thus γ6 TM1might function as a pore blocker. Also γ6 TM1a peptide inhibits Cav1.2 current with reduced efficacy. The γ6 TM1a peptide has the potential of being further developed as a novel therapeutic agent targeting Cav3.1 and possibly Cav1.2 calcium current.
SML2743 TM30089 ≥98% (HPLC) TM30089 is a ramatroban analog and an orally active, high-affinity, potent and selective prostaglandin D2 receptor 2 (DP2; CRTH2) antagonist (Ki = 0.6 nM/hDP2 against 1.2 nM PGD2; Ki = 1.2 μM/hDP1 against 0.5 nM PGD2, >10 μM/hTP against 5 nM SQ29548) that blocks PGD2-induced responses in hDP2 transfectants (IP1/βarr IC50 = 1.2/3.0 nM) and exhibits in vivo efficacy in a murine model of renal tubulointerstitial fibrosis (20 mg/kg b.i.d. p.o., starting 4 days before or 3 days after unilateral ureteral obstruction/UUO).
SML1398 TM5275 sodium salt ≥98% (HPLC) TMS5275 is an orally available, potent and selective inhibitor of PAI-1 that delivers antithrombotic benefits devoid of bleeding effect in nonhuman primates.
PZ0336 TMI-1 ≥98% (HPLC) TMI-1 (WAY-171318) is potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) also known as the tumor necrosis factor-α (TNF-α) converting enzyme (TACE), and matrix metalloprotease (MMP). TMI-1 potently inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood. TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines.
T5576 TMPH hydrochloride solid, (Product is pure based on CHN, NMR and MS results) 2,2,6,6-tetramethylpiperidin-4-yl heptanoate (TMPH) is a potent inhibitor of neuronal nicotinic receptors. Evaluation of nicotinic acetylcholine receptor (nAChR) subunits expressed in Xenopus laevis oocytes indicated that TMPH can produce a potent and long-lasting inhibition of neuronal nAChR formed by the pairwise combination of the most abundant neuronal alpha (i.e., alpha3 and alpha4) and beta subunits (beta2 and beta4), with relatively little effect, because of rapid reversibility of inhibition, on muscle-type (alpha1beta1gammadelta) or alpha7 receptors. However, the inhibition of neuronal beta subunit-containing receptors was also decreased if any of the nonessential subunits alpha5, alpha6, or beta3 were coexpressed. This decrease in inhibition is shown to be associated with a single amino acid present in the second transmembrane domain of these subunits. TMPH abilitty to relate the diverse central nervous system effects to specific nAChR subtypes makes it a useful tool for studying the functional roles of nAChR.
SML1698 TMPPAA ≥98% (HPLC) TMPPAA is an allosteric agonist and positive allosteric modulator (PAM) of 5-HT3 receptor. TMPPAA behaves as both an agonist and a PAM at 5-HT3A receptors, not via binding at the orthosteric site.
T7580 TN-16 ≥98% (HPLC) Inhibitor of microtubule assembly
TN-16 is a synthetic compound that blocks the assembly, and promotes the dissociation of microtubules. TN-16 has been shown to prevent the b-TrCP-mediated degradation of the transcription factor Gli2, leading to the up-regulation of BMP-2 and supporting a role for microtubule formation in the regulation of bone formation.
SML1711 TNCA ≥98% (HPLC) TNCA is a tryptophan derivative that binds the parathyroid Ca2+-sensing receptor (CaSR) extracellular domain (ECD) hinge region between two globular subdomains and acts as a high-affinity CaSR ligand (CaSRL) with co-agonist activity. TNCA is shown to potentiate both Mg++- and Ca++-evoked cellular calcium response (0.1-0.5 mM), as well as Mg++-evoked cellular ERK1/2 phosphorylation in CaSR-expressing HEK293 cells (0.5 mM). AC-265347 (Cat. No. SML0129), on the other hand, is a calcimimetic that functions as a CaSR agonist.
SML1472   TNIIIA2 trifluoroacetate salt ≥95% (HPLC) TNIIIA2 is a Tenascin-C driven proadhesive peptide that potently activates β1-integrins including α5β1. TNIIIA2 forces hematopoietic tumor cell lines to adhere via VLA-4 to fibronectin, which induces apoptosis. It appears that TNIIIA2 uses Syndecan-4 as a receptor.
T3955 TNP ≥95% (HPLC) TNP is a potent and selective IP6K inhibitor; less selective inhibitor of IP3K. Discovery of TNP as an inositol trisphosphate (IP3) kinase inhibitor was first reported in 2002, However, a recent reference shows that TNP is more potent as an IP6K inhibitor, making it valuable for study of inositol pyrophosphates.
T1455 TNP-470 ≥98% (HPLC) Studies have reported that TNP-470 can decrease intimal neovascularization in Apo-E deficient mice. TNP-470 can also prevent tumor growth in human breast and prostate cancer cell lines.
TNP-470 is a methionine aminopeptidase-2 (MetAP-2) inhibitor, selective for MetAP-2 over MetAP11. TNP-470 is an antiangiogenic.
T0202 Tocainide hydrochloride ≥98% (HPLC), solid Tocainide hydrochloride is a primary amine analog of lidocaine (lignocaine), used for the treatment of tinnitus. It blocks the sodium channels in the pain-producing foci in the nerve membranes and renders an analgesic effect in trigeminal neuralgia.
Tocainide hydrochloride is a sodium channel blocker; Class IB antiarrhythmic.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
T3251 (±)-α-Tocopherol synthetic, ≥96% (HPLC) Tocopherols (vitamin E) comprise of a series (α, β, γ and δ) of chiral compounds that differ by the methylation degree of the phenol moiety of the chromanol ring. They function as lipid soluble antioxidants and protect cell membranes from oxidative damage. α-tocopherols are favorably absorbed by humans and their nicotinate salts can function as vitamin E supplements. Studies have also reported that vitamin E can prevent cell damage caused by pharmacologically induced epilepsy in rats.
T6575 TOFA ≥98% (HPLC) 5-(Tetradecyloxy)-2-furoic acid (TOFA) elicits hypolipidemic functionality by favoring fatty acid breakdown and at the same time preventing biosynthesis. It induces apoptosis in pancreatic cancer cells and favors tumor suppression.
Studies have reported that TOFA can inhibit the anorectic effect of subcutaneous tamoxifen (TMX) on food intake during refeeding experiments in rats.
TOFA is a cell-permeable, potent, reversible, and competitive inhibitor of acetyl-CoA carboxylase (ACC). TOFA is a key enzyme involved in fatty acid biosynthesis. TOFA inhibits cellular fatty acid synthesis in a dose-dependent manner (IC50 = 4 μM in human breast cancer cell line MCF7).
PZ0017 Tofacitinib citrate ≥98% (HPLC) Tofacitinib is a potent inhibitor of Janus kinase 3 (JAK3) with some JAK-1 inhibitory activity as well. It blocks downstream STAT signaling resulting in potent inhibition of inflammatory cytokines with resultant immunosuppressive and anti-inflammatory activity. Tofacitinib is being investigated for for several autoimmune disorders including, rheumatoid arthritis, psoriasis and dry eye.
human ... JAK1(3716), JAK2(3717), JAK3(3718), TYK2(7297)
T8200 Tofisopam ≥98% (HPLC), solid Ligand for the GABAA receptor benzodiazepine modulatory site.
Studies have reported that tofisopam functions by blocking PDE4 (phosphodiesterase 4). Furthermore, the S-enantiomer of tofisopam is considered ten times more active than R-enantiomer.
SML0150 Tolcapone ≥98% (HPLC) Inhibition of catechol-O-methyltransferase by tolcapone increases the half-life and bioavailabilty of levodopa. It therefore is an effective adjunctive therapy in patients with Parkinson′s disease with motor response fluctuations.
Tolcapone is an orally active catechol-O-methyltransferase (COMT) inhibitor. It inhibits both central and peripheral COMT. Tolcapone crosses the blood-brain barrier, and has been used for L-DOPA adjunct therapy in the treatment of Parkinson′s Disease.
human ... COMT(1312)
JN0004 Tolmetin sodium dihydrate ≥98% (HPLC) Tolmetin sodium is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits prostaglandin synthetase in vitro and reduces plasma levels of prostaglandin E. Tolmetin sodium exhibits anti-inflammatory, analgesic and antipyretic activity Its precise mechanism of is unknown. Tolmetin is used to treat rheumatoid arthritis, osteoarthrosis, pain, and ankylosing spondylitis.
human ... PTGS1(5742), PTGS2(5743)
T3452 Toloxatone ≥98% (HPLC), solid Toloxatone is a reversible monoamine oxidase A inhibitor (MAOI) and antidepressant. Toloxatone belongs to the aryloxazolidinones, a relatively new class of reversible monoamine oxidase A inhibitors (MAOI). Studies show that derivatives such as 3-aryloxazolidin-2-one (oxazolidinones), which are regularly used to treat gram positive infections, represent a new class of reversible as well as irreversible inhibitors for MAO-A and MAO-B enzymes that are able to inhibit protein synthesis and also used for neurodegenerative-type pathologies.
T3577 Tolperisone hydrochloride ≥98% (HPLC), solid Tolperisone is an ion channel blocker and centrally acting muscle relaxant.
Tolperisone is derived from piperidine and possesses membrane stabilizing action. It helps in reducing the effect of spasticities associated with the nervous and muscular system. It exhibits muscle relaxant action through attenuating voltage-gated sodium channels in the brain stem.
Tolperisone regulates ionic currents in myelinates axons and subsequently decreases excitability and mediates its antispastic functions3.
SML1573   Tolrestat ≥98% (HPLC) Tolrestat is an orally active and potent aldose reductase inhibitor. Studies have also shown that it reduces RBC (red blood cells) sorbitol levels in rats.
Tolrestat is considered to be effective in treating the consequences of diabetes including neuropathy, nephropathy, retinopathy and esophageal motility and vibration perception. Tolrestat is also believed to have lesser or no toxic effects.
T7455 Tolvaptan ≥98% (HPLC), powder Tolvaptan (OPC 41061) is a potent, orally active non-peptide vasopressin V2 selective antagonist. IC50 = 3 nM at the rat V2 receptor; 29 times more selective for the V2 than for V1a. Tolvaptan has also been shown to inhibit the development of polycystic kidney disease in several animal models.
human ... AVPR2(554)
T7947 (R)-Tomoxetine hydrochloride solid Norepinephrine uptake blocker.
human ... SLC6A2(6530)
SML1354 Tonabersat ≥98% (HPLC) Tonabersat (SB-220453) exhibits anticonvulsant property. It is a member of the family of novel benzoylamino-benzopyran compounds. Tonabersat is used as a therapeutic for trigeminal nerve-induced neurovascular reflexes. In addition, it acts as a putative migraine prophylactic agent containing an unique stereospecific binding site in the brain.
Tonabersat is a potent inhibitor of neuronal-glial gap junctions in trigeminal ganglion that inhibits cortical spreading depression (CSD) and neurogenic inflammation in animal models of migraine.
T0575 Topiramate ≥98% (HPLC), solid Kainate GluR5 receptor antagonist; anticonvulsant.
Topiramate is a derivative of suphamate fructopyranose that inhibits the release of mesocorticolimbic dopamine. It facilitates GABA activity and inhibits glutamate function to alleviate the rewarding effects of alcohol. It modulates the trigeminovascular signaling that is effective in migraine prevention. Topiramate is structurally similar to fructose- 1,6-diphosphate and has the ability to inhibit the enzyme fructose 1,6-bisphosphatase, thereby preventing gluconeogenesis. It is found to inhibit the AMPA/kainate receptor-mediated signaling pathway in cultured neurons.
human ... CA1(759), CA2(760), CA4(762), CA5A(763), CA5B(11238), CA9(768), GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879), GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893), GRIK1(2897), GRIK2(2898), GRIK3(2899), GRIK4(2900), GRIK5(2901), SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
mouse ... Car5a(12352)
rat ... Car2(54231), Car4(29242)
T2705 Topotecan hydrochloride hydrate ≥98% (HPLC and enzymatic) Topotecan is a topoisomerase I inhibitor and an apoptosis inducer. It is a potent antineoplastic agent.
human ... TOP1MT(116447)
PZ0170 Torcetrapib ≥98% (HPLC) Torcetrapib is a Cholesteryl ester transfer protein (CETP) inhibitor. CETP normally transfers cholesterol from HDL cholesterol to very low density or low density lipoproteins (VLDL or LDL). Inhibition of this process results in higher HDL levels (the "good" cholesterol-containing particle) and reduces LDL levels (the "bad" cholesterol). Unfortunately clinical trials were stopped because of excessive all cause mortality. Reasons are still being investigated, but may be related to some off target effects such as an increase in aldosterone secretion not found in some other CETP inhibitors.
T7204 Toremifene citrate salt ≥98% (HPLC) Toremifene citrate is an oral selective estrogen receptor modulator (SERM). It is used in advanced (metastatic) breast cancer and being evaluated for prevention of prostate cancer. Toremifene citrate is known to increase bone mineral density in prostate cancer patients undergoing androgen deprivation therapy†.
human ... ESR1(2099), ESR2(2100)
SML1224   Torin2 ≥98% (HPLC) Torin2 is a highly potent and selective ATP-competitive mTOR inhibitor. Torin2 has an IC50 of 0.25 nM and 800-fold greater selectivity for mTOR than PI3K.
T3202 Torsemide ≥98% (HPLC), solid Torsemide functions in the thick ascending limb of the loop of Henle and enhances the excretion of sodium, chloride and water from the luminal side of the cells. Furthermore, torsemide can treat oedematous conditions that are associated with diseases such as liver cirrhosis, kidney disorders and chronic congestive heart failure2.
Torsemide is a loop diuretic of the pyridine-sulfonylurea class with antialdosteronergic properties and inhibitor of the Na+/K+/2Cl- carrier system.
human ... SLC12A1(6557)
SML2303 Tosedostat ≥98% (HPLC) Tosedostat (CHR-2797) is a potent cell permeable, antiproliferative aminopeptidase inhibitor. It has been in clinical trials for AML, pancreatic cancer and more.
T3580 Toyocamycin ≥98% (HPLC), from Streptomyces rimosus Studies have implicated that toyocamycin blocks the replication of fowl plague virus.
Toyocamycin is a nucleoside- type antibiotic analogue of adenosine, isolated from Streptomyces species. Toyocamycin is an anti-tumor antibiotic with various target activities. Toyocamycin is a potent inhibitor of RNA self-cleavage in mammalian cells. It also inhibits phosphatidylinositol kinase, a cell proliferation regulator. Toyocamycin was also found to inhibit Auxin signaling. Auxins are plant hormones with a crucial role in plant development regulation, and Toyocamycin was found to specifically inhibit auxin-responsive gene expression.
SML2252 TP053 ≥98% (HPLC) TP053 is a potent thienopyrimidine antitubercular agent that kills both replicating and nonreplicating Mycobacterium tuberculosis. It appears that TP053 is a prodrug, which is activated by mycothiol-dependent reductase Rv2466c.
SML2434 TP-238 Hydrochloride ≥98% (HPLC) TP-238 is a chemical probe for CECR2 (cat eye syndrome chromosome region, candidate 2), a gene expressed in the nervous system involved in neurulation, and for BPTF bromodomains. It has an activity of 10-30 nM with CECR2 and 100-350 nM with BPTF. TP-238 showed an IC50 of 30nM against CECR2 and 350nM against BPTF in an alphascreen assay and a KD of 10nM for CECR2 and 120nM for BPTF by ITC. The structurally related negative control TP-422 is completely inactive against BPTF and CECR2.
SML1862 TP-472 ≥98% (HPLC) TP-472 is a selective probe for bromodomain-containing proteins BRD9 and BRD7. This BRD9/7 probe was developed out of a collaborative effort by Takeda and the SGC, and is of a different chemotype from BRD9/7 probes previously available. TP-472 has a KD value of 33nM for BRD9 and 340nM for BRD7 by ITC. It is >30 fold selective for BRD9 over all other bromodomain family members except BRD7. It is suitable for in vivo applications. For full characterization details, please visit the TP-472 probe summary on the Structural Genomics Consortium (SGC) website.

TP-472N is used as a negative control and is available from Sigma. To learn more about and purchase TP-472N, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1933 TP-472N ≥98% (HPLC) TP-472N is a negative control probe for TP-472. TP-472 is a selective probe for bromodomain-containing proteins BRD9 and BRD7. The BRD9/7 probe was developed out of a collaborative effort by Takeda and the SGC, and is of a different chemotype from BRD9/7 probes previously available. TP-472 has a KD value of 33nM for BRD9 and 340nM for BRD7 by ITC, is >30 fold selective for BRD9 over all other bromodomain family members except BRD7, and is suitable for in vivo applications. The negative control TP-472N is inactive against other bromodomains (>20μM against BRD9). For full characterization details of TP-472 and TP-472N, please visit the TP-472 probe summary on the Structural Genomics Consortium (SGC) website.

TP-472, the active BRD9/7 probe, is available from Sigma. To learn more about and purchase TP-472, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML2447 TPA023 ≥98% (HPLC) TPA023 is a highly potent, functionally selective agonist for α2-, α3-, and α5GABAA receptors that shows zero efficacy at a1GABAA subtypes. TPA023 exhibits anxiolytic and anticonvulsant effects in both animals and humans but lacks sedative effects and abuse potential.
T5202 TPBM ≥98% (HPLC), solid TPBM is a potent inhibitor of estrogen receptor α via blocking ERα binding to consensus estrogen response element (cERE) DNA. Estrogen receptor α (ERα) plays an important role in several human cancers. Current ERα antagonists bind in the receptor ligand binding pocket and compete for binding with estrogenic ligands. TPBM instead inhibits ERα via binding to consensus estrogen response element (cERE) DNA. TPBM is not toxic to cells and does not effect estrogen-independent cell growth. TPBM does not act by chelating the zinc in ERs zinc fingers and differs from known ERα inhibitors.
T1452 TPCA-1 ≥95% (HPLC) TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.
T6205 TPh A ≥98% (HPLC) TPh A is an inhibitor of the nuclear protein pirin. TPh A (Triphenyl compound A) inhibits the interaction between Bcl3 oncoprotein and the nuclear protein pirin. TPh A inihibits melanoma cell migration.
SML0750   TPPU ≥98% (HPLC) TPPU is a potent sEH inhibitor (IC50 = 3.7 nM) that has been shown to have very favorable PK attributes in cynomolgus monkeys. sEH converts epoxyeicosatrienoic acids (EETs) to dihydroxyiecosatrienoic acids (DHETs), and sEH inhibitors display anti-inflammatory and anti-atherosclerotic effects.
SML0232   TPSF ≥98% (HPLC) TPSF is a noncompetitive, potent inhibitor of estrogen receptor α, that does not compete with estrogen for binding to Erα. The compound has low toxicity and selectively targets E2-ERα-dependent cell growth. TPSF is effective in cells that become tamoxifen-resistant. It appears that down-regulation of ERα by TPSF is at list partially dependent to enhancement of proteasome-dependent degradation of ERα.
SML1065 TR100 ≥98% (HPLC) TR100 is a specific anti-tropomyosin agent that preferentially disrupts the actin cytoskeleton of tumor cells. TR100 selectively disrupts Tm5NM1/2 containing actin filaments. TR100 induces apoptosis in a panel of neural crest-derived tumor cell lines with no adverse effects on cardiac structure and function.
T6700 TRAM-34 ≥98% (HPLC), solid TRAM-34 exhibits 100-fold selectivity (Kd = 20 nM) for IKCa1 channels over other K+ channels (Charybdotoxin, Kd = 5 nM, Clotrimazole, Kd = 70 nM; Nitrendipine Kd = 900 nM). Furthermore, TRAM-34 is known to suppress the activation of human T lymphocytes,.
TRAM-34 is a potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel.
T4827 Trandolapril ≥98% (HPLC), white powder Studies have reported that trandolapril inhibits atherosclerosis1 and decreases the occurrence of atrial fibrillation2.
Trandolapril is an ACE inhibitor. Trandolapril differs from other ACE inhibitors in that it has a longer biological half-life and a high degree of lipophilicity.
human ... ACE(1636)
T0318 Tranilast ≥98% (HPLC), powder Tranilast also inhibits vascular smooth muscle cell proliferation by inhibiting the cyclin-dependent kinase inhibitor-1(p21Waf1/Cip1) and may be useful in treating cardiac allograft vasculopathy. It is used in treating hypertrophic scars and keloids. Tranilast inhibits tumor necrosis factor (TNF-α and TGF-β2), obstructing epithelial-mesenchymal transition in human retinal pigment epithelial cell line (ARPE).
Tranilast is an anti-asthma drug, which inhibits LTC4 and PGE2 formation in stimulated monocytes, but does not inhibit cyclooxygenase or lipoxygenase activity; inhibits mast cell degranulation; inhibits VEGF-induced angiogenesis in vivo and also inhibits proliferation and tube formation of human endothelial cells in vitro. Tranilast may represent a new class of drugs for therapy to treat ongoing TH1-mediated autoimmune diseases.
human ... VEGFA(7422), VEGFB(7423), VEGFC(7424)
T5830 Trap-101 hydrochloride ≥98% (HPLC), powder Trap-101 Hydrochloride is a nociceptin/orphanin FQ peptide (NOP) receptor blocker. Trap-101 acts as an inverse agonist. Trap-101 had been found to be an effective NOP receptor antagonist both in vitro and in vivo, with equivalent potency to J113397.