SML1422
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CCG-203971 ≥98% (HPLC)
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CCG-203971 is an inhibitor of the Rho/MKL1/SRF transcriptional pathway, which has been shown to play a role in metastasis of melanoma and breast cancer and clinically associated with castration-resistant prostate cancer. CCG-203971 is a second-generation analog of CCG-1423 (SML0987) with an IC50 of 4.2 μM vs 1 μM for CCG-1423, but less cytotoxicity. In mouse studies, CCG-203971 inhibited invasion of PC-3 prostate cancer cells and was well tolerated up to doses of 100 mg/kg IP over 5 days.
The Rho/MRTF/SRF pathway has also been shown to be involved in multiple types of solid organ fibrosis. CCG-203971 repressed both matrix-stiffness and TGF-β-mediated fibrogenesis in human colonic myofibroblasts and showed antifibrotic activity in a murine model of skin injury and in pulmonary fibrosis lung fibroblasts.
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SML1052
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2-D08 ≥98% (HPLC)
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2-D08 is a potent and cell-permeable inhibitor of sumoylation that block the transfer of SUMO (small ubiquitin-like modifier) from the E2 enzyme (Ubc9) thioester conjugate to the substrate.
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D5321
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D36 hydrate ≥98% (HPLC)
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D36 is an androgen receptor (AR) allosteric antagonist with inverse agonist properties. D36 inhibits both wild-type and agonist-induced AR activity and antagonized AR in a hormone-refractory model.
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SML2256
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D3-βArr ≥98% (HPLC)
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D3-βArr is a positive allosteric modulator of TSHR (thyrotropin receptor) for β-Arr 1-mediated signaling that initiates translocation of β-Arr 1 by direct TSHR activation, while showing no agonistic effect on cAMP production. D3-βarr is a positive allosteric modulator for TSH-enhanced osteoblast differentiation.
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D1944
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D4476 ≥98% (HPLC), solid
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D4476 is a potent, selective ATP-competitive inhibitor of CK1 (casein kinase 1). D4476 may prevent or enhance apoptosis. It triggers tumor suppressor p53 and impairs transcription factor E2F-1.
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SML2865
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D5D-IN-326 ≥98% (HPLC)
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D5D-IN-326 (Compound-326) is an orally available, potent and selective inhibitor of delta-5 desaturase (D5D) that reduces insulin resistance and body weight in a high-fat diet-induced obese mice. It appears that D5D-IN-326 significantly inhibits the progression of atherosclerosis in the aorta of western-diet fed ApoE knockout (KO) mice. It is called Compound-326 in recent J Pharmacol Exp Ther. 2019 Nov;371(2):290-298. (PMID: 31488602) paper.
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SML2975
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Dabcyl-KTSAVLQSGFRKME-Edans trifluoroacetate ≥95% (HPLC)
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Dabcyl-KTSAVLQSGFRKME-Edans is a fluorescence resonance energy transfer (FRET) substrate for SARS-CoV main protease Mpro (also called 3CLpro) (538 nm with excitation at 355 nm). Dabcyl-KTSAVLQSGFRKME-Edans is suitable to measure protease activity of COVID-19 virus Mpro, SARS-CoV Mpro, and other viruses.
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SML2370
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Dabigatran ≥95% (HPLC)
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Dabigatran is a nonpeptide direct thrombin inhibitor. It is an anticoagulant that functions by directly inhibiting both free and fibrin-bound thrombin. Dabigatron has been shown to prevent strokes in those with atrial fibrillation not caused by heart valve issues.
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SML2351
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Dabigatran etexilate ≥98% (HPLC)
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Dabigatran etexilate is a prodrug of dabigatran, a nonpeptide direct thrombin inhibitor. Dabigatron is an anticoagulant that functions by directly inhibiting both free and fibrin-bound thrombin. Dabigatron has been shown to prevent strokes in those with atrial fibrillation not caused by heart valve issues.
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SML0736
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Dafadine A ≥98% (HPLC)
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Dafadine A is a selective inhibitor of C. elegans DAF-9 cytochrome P450, a key regulator of dauer formation, developmental timing and longevity. C. elegans has four life stages. In harsh environmental conditions, nematodes can convert to the L3 stage, known as the ""non-aging"" dauer stage, in which development ceases until improved conditions are sensed. Dafadine A can induce dauer formation and increased longevity in wild-type worms raised in nonstressful conditions. Dafadine A is the only inhibitor known to robustly inhibit DAF-9 in wild-type worms. It does not inhibit DAF-12 activity. Dafadine is active in mammalian systems, inhibiting CYP27A1, the mammalian functional ortholog of DAF-9 that oxidizes 4-cholesten-3-one to make 26-hydroxy-4-cholesten-3-one and Δ4-dafachronic acid, without inhibiting other sterol- and oxysterol-metabolizing P450s such as CYP7A1 or CYP7B1.
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D1821
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DAF-FM ≥98% (HPLC)
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DAF-FM is a highly sensitive, photo-stable fluorescent probe for the detection of nitric oxide (NO). DAF-2 is the original compound and is widely used, but DAF-FM is more sensitive to nitric oxide (NO) compared with DAF-2. DAF-FM is more photo-stable and less pH sensitive than DAF-2. DAF-FM is not quite as cell-permeable as the diacetate derivative, DAF-FM, but it does not need to be activated by cytosolic enzymes.
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D1946
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DAF-FM DA ≥98% (HPLC)
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DAF-FM DA is a cell-permeable fluorescent probe for the detection of nitric oxide (NO). DAF-2 is the original compound and is widely used, but DAF-FM and DAF-FM DA are more sensitive to nitric oxide (NO) compared with DAF-2 and more photo-stable and less pH sensitive. DAF-FM DA permeates well into living cells and is rapidly transformed into water-soluble DAF-FM by cytosolic esterases.
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D2321
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DAF-FM DA solution 5 mM in DMSO, ≥97% (HPLC)
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DAF-FM DA is a cell-permeable fluorescent probe for the detection of nitric oxide (NO). DAF-2 is the original compound and is widely used, but DAF-FM and DAF-FM DA are more sensitive to nitric oxide (NO) compared with DAF-2 and more photo-stable and less pH sensitive. DAF-FM DA permeates well into living cells and is rapidly transformed into water-soluble DAF-FM by cytosolic esterases.
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D2196
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DAF-FM solution 5 mM in DMSO, ≥97% (HPLC)
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DAF-FM is a highly sensitive, photo-stable fluorescent probe for the detection of nitric oxide (NO). DAF-2 is the original compound and is widely used, but DAF-FM is more sensitive to nitric oxide (NO) compared with DAF-2. DAF-FM (Ex: 500 nm; Em: 515 nm; dectection limit: 3 nM) is more photo-stable and less pH sensitive than DAF-2. DAF-FM is not quite as cell-permeable as the diacetate derivative, but it does not need to be activated by cytosolic enzymes.
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SML2378
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Dalbavancin ≥90% (HPLC)
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Dalbavancin is a semisynthetic, vancomycin class lipoglycopeptide with antibacterial activity against a variety of gram-positive pathogens, including methicillin-resistant S. aureus & S. epidermidis (MRSA & MRSE), but not gram-negative or vancomycin-resistant enterococci that possess VanA gene. Similar to vancomycin and other class members (e.g. teicoplanin, telavancin, ramoplanin, and ritavancin), dalbavancin disrupts bateria cell wall formation and cell membrane integrity by targeting the D-alanyl-D-alanyl residues on the growing peptidoglycan chains, blocking transpeptidation and peptidoglycan elongation.
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SML2091
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Dalcetrapib ≥97% (HPLC)
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Dalcetrapib is a cholesteryl ester transfer protein (CETP) inhibitor. It increases HDL levels, but showed variable results on clinical outcomes. Clinical outcomes, effects on C-reactive protein and cholesterol efflux have been found to be genotype-dependent, influenced by correlated polymorphisms in the ADCY9 (adenylate cyclase type 9) gene. Positive results were obtained with AA genotype of ADCY9 gene whereas the GG genotype showed negative results and the AG genotype was neutral.
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D7441
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Daltroban >98% (HPLC)
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Selective thromboxane A2 receptor antagonist
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human ... TBXA2R(6915)
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SML0255
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4-DAMP ≥98% (HPLC)
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4-DAMP is a M3 preferring cholinergic receptor antagonist.
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D8399
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Danazol ≥98%
|
Danazol is a weak androgen; anterior pituitary suppressant.
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SML0679
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Danshensu sodium salt ≥98% (HPLC)
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Danshensu is an active component of Salvia miltiorrhiza (Danshen) that suppresses the formation of reactive oxygen species, inhibits platelet adhesion and aggregation, and protects myocardium against ischemia. Danshensu is cardioprotective, which protects myocardium from the reperfusion injury and inhibits apoptosis of H9c2 cardiomyocytes via Akt and ERK1/2 phosphorylation.
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D9175
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Dantrolene sodium salt
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Inhibitor of Ca2+ release from sarcoplasmic reticulum; muscle relaxant.
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human ... RYR1(6261), RYR3(6263)
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SML2804
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Dapagliflozin ≥98% (HPLC)
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Dapagliflozin (BMS-512148) is an orally active, potent and selective renal sodium-dependent glucose cotransporter 2 (SGLT2; SLC5A2) inhibitor (human/rat SGLT2 IC50 = 1.1/3 nM vs. human/rat SGLT1 IC50 = 1.39/0.6 μM; R-methyl-D-glucopyranoside (AMG) uptake assay with respective CHO transfectants). Dapagliflozin reduces blood glucose levels (by 55% in streptozotocin (STZ)-induced hyperglycemic rats 5 hrs post 0.1 mg/kg p.o.) by preventing the renal glucose reabsorption process and promoting glucose excretion in urine with good pharmacokinetic properties and oral availability (84% in rats and 83% in dogs, respectively, post 1 mg/kg and 6.6 mg/kg p.o.) in vivo.
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SML2758
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Dapagliflozin propanediol monohydrate ≥98% (HPLC)
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Dapagliflozin (BMS-512148) is an orally active, potent and selective renal sodium-dependent glucose cotransporter 2 (SGLT2; SLC5A2) inhibitor (human/rat SGLT2 IC50 = 1.1/3 nM vs. human/rat SGLT1 IC50 = 1.39/0.6 μM; R-methyl-D-glucopyranoside (AMG) uptake assay with respective CHO transfectants). Dapagliflozin reduces blood glucose levels (by 55% in streptozotocin (STZ)-induced hyperglycemic rats 5 hrs post 0.1 mg/kg p.o.) by preventing the renal glucose reabsorption process and promoting glucose excretion in urine with good pharmacokinetic properties and oral availability (84% in rats and 83% in dogs, respectively, post 1 mg/kg and 6.6 mg/kg p.o.) in vivo.
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D3943
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DAPH ≥98% (HPLC), solid
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DAPH is an inhibitor of Aβ fibril formation; Protein tyrosine kinase inhibitor, specific for EGFR.
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human ... EGFR(1956)
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SML1610
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Dapiprazole hydrochloride ≥98% (HPLC)
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Dapiprazole hydrochloride is an an α-adrenergic blocking agent that is used to reverse mydriasis after eye examination.
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human ... ADRA1A(148)
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D7071
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Dapoxetine hydrochloride ≥98% (HPLC)
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Dapoxetine is capable of blocking recombinant Kv4.3 potassium voltage-gated channels. It is considered as safe. Potent Selective serotonin reuptake inhibitor (SSRI); used in treatment of premature ejaculation
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human ... SLC6A4(6532)
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D5942
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DAPT ≥98% (HPLC), solid
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DAPT is a γ-secretase inhibitor and indirectly an inhibitor of Notch, a γ-secretase substrate. Other γ-secretase substrates include LDL receptor-related protein, E-cadherin and ErbB-4. As an inhibitor of γ-secretase, DAPT may be useful in the study of β-amyloid (Aβ) formation. DAPT has been shown to inhibit Notch signaling in studies of autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE), as well as in cancer cell growth, angiogenesis, and differentiation of human induced pluripotent stem cells (hIPSC).
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human ... APH1A(51107), APH1B(83464), NCSTN(23385), NOTCH1(4851), NOTCH2(4853), NOTCH3(4854), NOTCH4(4855), PSEN1(5663), PSEN2(5664), PSENEN(55851) mouse ... Aph1a(226548), Aph1b(208117), Ncstn(59287), Notch1(18128), Notch2(18129), Notch3(18131), Notch4(18132), Psen1(19164), Psen2(19165), Psenen(66340) rat ... Aph1a(365872), Aph1b(300802), Ncstn(289231), Notch1(25496), Notch2(29492), Notch3(56761), Notch4(406162), Psen1(29192), Psen2(81751), Psenen(292788)
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SML0977
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Darglitazone sodium salt ≥98% (HPLC)
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Darglitazone is a highly potent and selective PPAR-γ (peroxisome proliferator-activated receptor-γ) agonist. Darglitazone is a thiazolidinedione approximately 200x more potent than ciglitazone. Darglitazone restores euglycemia and reduced circulating TG and VLDL in the ob/ob mice. Also Darglitazone offers a significant neuroprotection and promotes recovery after a hypoxic-ischemic insult in the diabetic ob/ob mouse.
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SML1102
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Darifenacin hydrobromide ≥98% (HPLC)
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Darifenacin hydrobromide is an antispasmodic muscarinic antagonist, selective for blocking the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions. Darifenacin hydrobromide has 9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4. Darifenacin is used clinically to treat urinary incontinence and overactive bladder syndrome. Darifenacin hydrobromide is an antispasmodic muscarinic antagonist, selective for blocking the M3 muscarinic acetylcholine receptor.
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human ... CHRM2(1129), CHRM3(1131)
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SML0937
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Darunavir ≥98% (HPLC)
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Darunavir has been sanctioned by the food and drug administration (FDA) as the first treatment of drug-resistant human immunodeficiency virus (HIV). Darunavir is a second-generation antiviral HIV protease inhibitor with broad spectrum activity.
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SML2853
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DASA-58 ≥98% (HPLC)
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DASA-58 is a potent and selective activator of cancer-specific pyruvate kinase isoform PKM2 (hPKM2 AC50 = 38 nM, Emax = 82%), but not PKM1, PKR or PKL, that stabilizes PKM2 tetrameric conformation by targeting a site distinct from that of fructose-1,6-bis-phosphate (FBP). DASA-58 exhibits good aqueous solubility (51.2 μg/mL), decreases cellular lactate production and suppresses cell proliferation selectively under hypoxic conditions (30 μM; H1299, 1% O2). When administered in mice, DASA-58 is reported to exhibit anti-thrombotic efficacy in vivo (40 mg/kg via iv).
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SML2589
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Dasatinib ≥98% (HPLC)
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Dasatinib is an orally available and highly potent pan-Src/Bcr-Abl inhibitor (Ki values are 16 and 30 pM, respectively. It also inhibits Lck, Fyn, c-kit and Yes with IC50 values in the subnanomolar range. Dasatinib exhibits potent antitumor activities and is used for treatment of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL).
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human ... ABL1(25), BLK(640), EPHA2(1969), FGR(2268), FRK(2444), FYN(2534), HCK(3055), KIT(3815), LCK(3932), LYN(4067), PDGFRB(5159), SRC(6714), SRMS(6725), YES1(7525)
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SML0597
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Daurisoline ≥98% (HPLC)
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Daurisoline alkaloid isolated from the rhizomes of Menispermum dauricum that exhibit varies pharmacological activities including antiplatelet aggregation, anti-inflammatory, neuron-protective properties, and antiarrhythmic effect. It appears that antiarrhythmic effect of daurisoline is maintained through blockade of hERG channels. Daurisoline is antiarrythmic, anti-inflammatory, neuron-protective; and blocks hERG channels.
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SML2063
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Davunetide trifluoroacetate salt ≥95% (HPLC)
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Davunetide (NAPVSIPQ; NAP) is an eight amino acid peptide identified as the active component of activity-dependent neuroprotective protein (ADNP). It has been found to be neuro-protective at femtomolar concentrations in vitro against the neural toxicity of a wide range of compounds. Davunetide has been investigated for Parkinson′s disease and schizophrenia and in clinical trials for Alzheimner′s Disease, targeting microtubule-tau Interaction.
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SML0031
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DBeQ ≥98% (HPLC)
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DBeQ is a potent and specific inhibitor of ATPase p97, an integral component of the ubiquitin-fusion degradation (UFD) pathway. DBeQ inhibits the degradation of ubiquitinated proteins, the endoplasmic reticulum-associated degradation pathway, and autophagosome maturation. The compound also potently inhibits cellular proliferation and induces caspase 3/7 activity and apoptosis.
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SML2687
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dBET1 ≥98% (HPLC)
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dBET1 is a JQ1-and-phthalimide conjugate that causes the degradation of BRD4 protein, a transcriptional coactivator that regulates the expression of genes that promote cancer cell proliferation and survival. JQ1 is a selective BET bromodomain (BRD) inihbitor. The phthalimide portion is a derivative of the drug thalidomide, which is known to bind to cereblon (CRBN), part of an ubiquitin E3 ligase complex resulting in ubiquitylation and degradation by the proteasome. The conjugate dBET1 induced highly selective cereblon-dependent BET protein degradation both in vitro and in vivo. It induced complete CRBN-dependent proteosomal degradation of BRD4 in a human acute myeloid leukaemia (AML) cell line and delayed leukemia progression in mice.
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SML2683
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dBET6 ≥98% (HPLC)
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dBET6 is a highly cell penetrant, potent and selective BET (bromodomain and extra-terminal domain) degrader that induces rapid (<4hrs) degradation of BRD2, BRD3 and BRD4 and complete down-regulation of c-MYC protein and induction of apoptosis. dBET6 exhibits potent anti-cancer activities.
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D7938
|
|
DBO-83 solid
|
Novel nicotinic acetylcholine receptor agonist, structurally related to epibatidine, with antinociceptive properties in rodents.
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human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143)
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SML2911
|
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dBRD9 Hydrochloride ≥97% (HPLC)
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dBRD9 is a cell permeable, potent and selective BRD9-directed chemical degrader that bridges the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex. dBRD9 exhibits a potent anti-proliferative activity in human AML lines.
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SML1512
|
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DC_05 ≥98% (HPLC)
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DC_05 is a potent and selective non-nucleoside DNMT1 (DNA methyltransferase 1) inhibitor that significantly inhibits cancer cell proliferation.
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SML1050
|
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DC260126 ≥98% (HPLC)
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DC260126 is a FFA1 (GPR40) selective antagonist. In FFA1-expressing CHO cells, DC260126 blocks linoleic acid-induced Ca2+ elevation and ERK phosphorylation (IC50 = 6028 μM), as well as palmitic acid potentiated glucose-stimulated insulin secretion. The compound DC260126 blocks MIN6 β cells from palmitic acid-induced ER stress and apoptosis.
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SML1640
|
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DC_AC50 ≥98% (HPLC)
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DC_AC50 is an inhibitor of copper trafficking proteins Atox1 and CCS, resulting in a disruption of cellular copper transport. Cancer cells rely more heavily on Atox1 and CCS than normal cells. DC_AC50 blockade of copper trafficking induces cellular oxidative stress, affecting cancer cells more strongly than normal cells, and leading to the inhibition of cancer cell proliferation.
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SML1714
|
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DCAI ≥95% (HPLC)
|
DCAI, an Inactive Ras, is bound to a GDP and activated by SOS (son of sevenless, among others), which converts it to the active GTP form. DCAI is a known binder to Ras, which inhibits SOS nucleotide exchange, inhibiting Ras activation.
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SML0515
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DCAP ≥95% (HPLC)
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DCAP is a potent broad-spectrum antibiotic that specifically targets the membranes of both Gram-positive and Gram-negative bacteria. It reduces the transmembrane potential, kills stationary-phase cells and sterilizes bacterial biofilms. DCAP has no effect on red blood cell membranes at levels toxic to bacteria.
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D1068
|
|
DCB ≥98% (HPLC), solid
|
3,3′-dichlorobenzaldazine (DCB) serves as an allosteric ligand with neutral cooperativity. It helps to block the positive allosteric regulation of mGluRs (metabotropic glutamate receptor subtype 5 (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB) and the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB). Neutral allosteric modulator of the metabotropic glutamate receptor mGluR5.
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SML2875
|
|
DCC-2618 ≥98% (HPLC)
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DCC-2618 is an orally active, potent type II switch pocket (SP) inhibitor against c-KIT (IC50 = 4 nM/WT, 8 nM/V654A, 18 nM/T670I, 5 nM/D816H, 14 nM/D816V) and PDGFR. DCC-2618 locks c-KIT & PDGFR in an inactive conformation and is effective against multiple clinical forms of mutations resistant to type I ATP (catalytic)-site inhibitors Imatinib and Sunitinib. DCC-2618 inhibits cellular c-KIT activation (IC50 = 36 nM/WT, 2 nM/ex 11 del, 7 nM/ex 11 del & V654A, 53 nM/V560D & D820A) and is efficacious against KIT mutants-mediated cancer growth in cultres (IC50 = 2 nM; GIST with KIT D816Y) and in mice in vivo (50 mg/kg b.i.d. p.o.; GIST with KIT delW557K558/Y823D, AML with KIT N822K).
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D9190
|
|
DCEBIO ≥98% (HPLC), solid
|
DCEBIO facilitates Cl− secretion in the epithelia by activating K+ and Cl− currents.
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human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
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D5569
|
|
DCHC ≥98% (HPLC), solid
|
DCHC is a SIRT1 activator. It increases peroxisome proliferator-activated receptor gamma co-activator 1α (PGC1α) expression, resulting in mitochondrial biogenesis. DCHC activates SIRT1 at low micromolar concentrations (5–10 μM) and increases SIRT1 activity at 100 μM. It is different from 5,7,4′-T in that it induces the activation of recombinant SIRT1, but does not increase SIRT1 expression.
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SML2692
|
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DCPIB ≥98% (HPLC)
|
DCPIB is a potent inhibitor of the volume-sensitive anion channel (VSAC). IC50 = 4.1μM ) versus ICl,swell in calf pulmonary artery endothelial (CPAE) cells. DCPIB does not inhibit CPAE cell ICl,Ca; hCFTR; nor guinea pig ICl,PKA, IKr, IKs,IKl, INa and ICa. DCPIB inhibition is reversible and voltage independent. ICl,swell is believed to be important in cardiovascular function. Studies have been limited by the lack of specific ligands. DCPIB is a reversible and highly selective volume-regulated anion channel (VRAC or VSOAC) blocker (by 50/98.7% of hypotonic solution-induced Cl current or ICl,swell at 4.1/10 μM in calf pulmonary artery endothelial (CPAE) cells vs. 4.1% inhibition of Ca2+-activated ICl,Ca or CaCC at 10 μM) with little or no inhibition against hminK (IKs), hCFTR, hCLC-1/2/4/5, rCLC-K1, hKv1.5, hKv4.3, HERG (≤5.9% at 10 μM; transpected xenopus oocytes), nor IKs, IKr, IK1, INa, ICa, or ICl,PKA in isolated guinea pig cardiomyocytes. When applied in rats in vivo (10 mg/kg ip.), DCPIB is shown to protect against myocardial ischaemia/reperfusion injury.
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D5318
|
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DCP-LA ≥95% (HPLC), oil
|
DCP-LA is a selective PKC-epsilon (PKC-ε) activator. In the in situ PKC assay with a reversed phase high-performance liquid chromatography, DCP-LA significantly activated PKC in PC-12 cells in a concentration (10 nM-100 μM)-dependent manner, with the maximal effect at 100 nM. DCP-LA has over a 7-fold greater potency for activation of PKC-ε over other PKC isozymes.
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SML0490
|
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DDN ≥98% (HPLC)
|
DDN (5,8-Diacetyloxy-2,3-dichloro-1,4-naphthoquinone) is a selective insulin receptor (IR) activator that binds directly to the receptor kinase domain and induces the Akt and ERK phosphorylations. DDN also improves glucose uptake in adipocytes and produces oral hypoglycemic effect in wild-type and diabetic mice models.
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SML2274
|
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DDR1-IN-1 ≥98% (HPLC)
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DDR1-IN-1 is a type II, subtype-selective discoidin domain receptor (DDR) tyrosine kinase inhibitor (DDR1/2 IC50 = 105 nM/413 nM) that effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture (123%, 70%, 50% of control, respectively, post 48-hr 250 nM DDR1-IN-1, 82.5 nM GSK2126458, or combined treatment). ent). ned treatment). DDR1-IN-1 protects cells from apoptosis by inhibiting collagen-mediated Bcl-2-interacting killer (BIK) induction at both mRNA and protein levels.
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SML1832
|
|
DDR1 Inhibitor 7rh ≥98% (HPLC)
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DDR1 Inhibitor 7rh is an orally available, potent, ATP-competitive DDR1-selective inhibitor with in vitro and in vivo anti-cancer efficacy. Compound 7rh is a potent, high affinity (Kd =0.6 nM), ATP-competitive inhibitor against discoidin domain-containing receptor 1 (DDR1; IC50 = 6.8 nM, [ATP] = 100 nM) with significantly reduced potency toward 455 other kinases, including DDR2, Bcr-abl, and c-Kit (IC50 = 101.4 nM, 355 nM and >10 μM, respectively). Inhibitor 7rh reduces DDR1 expression/phosphorylation and downstream signaling in a dose-dependent manner (0.1-2 μM; NCI-H23 NSCLCs), effectively suppressing human cancer cells proliferation (IC50 from 38 nM/K562 to 2.98 μM/NCI-H460) and colony formation (IC50 = 0.56 μM/NCI-H23). Inhibitor 7rh is orally availabe in rats and mice (T1/2 = 15.53 h; Tmax = 4.25 h; Cmax = 1867.5 μg/L, F = 67.4%; 25 mg/kg; rats) and displays in vivo efficacy against Kras (LSLG12Vgeo) tumor growth in mice (50 mg/kg/day p.o.).
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SML0710
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DDRI-18 ≥98% (HPLC)
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DDRI-18 (DNA Damage Response Inhibitor-18) inhibits nonhomologous end-joining (NHEJ) DNA repair following double strand DNA breaks induced by ionizing radiation, and enhances the effects of DNA-damaging cancer drugs like etoposide, camptothecin and doxorubicin.
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SML2526
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DDR-TRK-1 ≥98% (HPLC)
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DDR-TRK-1 was shown to inhibit the kinase activity of Discoidin Domain Receptor 1 (DDR1) with an IC50 value of 9.4 nM. DDR receptors are linked to the progression of various human diseases, including fibrotic disorders such as pulmonary fibrosis, as well as atherosclerosis and cancer. DDR-TRK-1 showed a therapeutic effect in a mouse model of pulmonary fibrosis and inhibited Panc-1 pancreatic cancer cell colony formation and migration. DDR-TRK-1 also inhibits the TRK family kinases TRKA, TRKB, and TRKC, which are selectively expressed in neuronal tissue. DDR-TRK-1N is the negative control compound.
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D8296
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3-Deazaadenosine
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Possesses antiviral activity inhibitor of leukocyte adhesion to TNF-treated endothelial cells.
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rat ... Adora1(29290), Adora2a(25369), Adora3(25370)
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SML0305
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3-Deazaneplanocin A hydrochloride ≥97% (HPLC)
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3-Deazaneplanocin A (DZNep) is an S-Adenosylhomocysteine Hydrolase inhibitor and histone methyltransferase EZH2 inhibitor. It switches on repressed tumor suppressor genes and induces apoptosis by inhibiting the expression of EZH2.
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D1260
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Decamethonium bromide crystalline
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Decamethonium serves as a muscle relaxant and is also a neuromuscular blocking agent. It has a molecular weight of 258.4. Nicotinic acetylcholine receptor partial agonist and neuromuscular blocking agent; depolarizes striated muscles and blocks their activity.
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human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143), CHRND(1144), CHRNE(1145), CHRNG(1146)
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SML0786
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Decursin ≥97% (HPLC)
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Decursin is a cumarin isolated from Radix peucedani that exhibits a number of physiological actions including anticancer, antibacterial, antinematodal and antioxidant. Decursin is potent anti-angiogenic agent targeting the VEGFR-2 signaling pathway. Decursin exhibits potent neuroprotective activity against glutamate and Ab- induced neurotoxicity. Apparently, decursin stimulates activation of Nerf2. Also, decursin inhibits androgen stimulated AR translocation to the nucleus in LNCaP prostate cancer cells.
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SML2673
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Deferasirox ≥98% (HPLC)
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Deferasirox is an orally available iron chelator used clinically for reduction of chronic iron overload in diseases such as β-thalassemia.
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SML0123
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Deflazacort ≥98% (HPLC)
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Deflazacort is an anti-inflammatory and immunosuppressant glucocorticoid.
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human ... NR3C1(2908)
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SML2856
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Degarelix acetate ≥98% (HPLC)
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Degarelix acetate (FE200486) is a gonadotropin-/luteinizing hormone-/follicle-stimulating hormone-releasing hormone (GnRH, LHRH, FSH-RH) receptor antagonist that inhibits plasma testosterone for more than 40 days following a single s.c. dosage of 2 mg/kg in rats and monkeys, showing longer in vivo duration than abarelix, ganirelix, cetrorelix, azaline B or D-Trp6-LHRH, and exhibiting only weak histamine-releasing potency in isolated rat mast cells. Bi-weekly s.c. dosing (2 mg/kg) is efficacious in suppressing the growth of human prostate cancer PAC120 xenograft-derived tumors in mice in vivo.
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D0817
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(−)-Deguelin >98% (HPLC), powder
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Inhibitor of activated Akt. Does not affect MAPK, ERK1/2, or JNK. Anticancer, chemoprotective agent.
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D2154
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5,6-Dehydroarachidonic acid ≥98%, ethanol solution
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Inhibits 5-lipoxygenase of guinea pig leukocytes with an IC50 of 10 μM. In extracts of rat basophilic leukemia cells preincubated with 5,6-dehydro AA, the Ki for the conversion of arachidonic acid to 5-HPETE is 15 μM.
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D5297
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Dehydroisoandrosterone 3-sulfate sodium salt dihydrate ≥93% (TLC), powder
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Dehydroisoandrosterone 3-sulfate sodium salt dihydrate is a negative allosteric modulator of GABAA receptors.
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human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
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D4196
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Dehydroleucodine ≥98% (HPLC)
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Dehydroleucodine is a sesquiterpene lactone isolated from Artemisia douglasiana Besser; mast cell stabilizers. An extract from the plant is widely used in Cuyo region (Argentina) as folk medicine for the treatment of gastric ailments. The compound prevents gastric and duodenal damages in response to necrosis-inducing agents. Stabilization of mast cells may be a key mechanism to protect the gastrointestinal tract from injury and ulceration. Recently, it was established that dehydroleucodine and xanthatin inhibit mast cell degranulation induced by compound 48/80.
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D4875
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16-Dehydropregnenolone acetate ≥95%
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16-Dehydropregnenolone acetate (DPA) is synthesized from steroids sapogenin, diosgenin and solasodine. 16-Dehydropregnenolone acetate (DPA) is a crucial intermediate for the synthesis of steroid hormones-based drugs. It is an antagonist for farnesoid X receptor (FXR) and modulates cholesterol metabolism. It is considered as a potential antihyperlipidemic agent. Chemically synthesized steroid derivatives from DPA have cytotoxic features and could serve as potential anticancer agents.
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SML2913
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Dehydroxylcannabidiol ≥98% (HPLC)
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Dehydroxylcannabidiol (DH-CBD) is a synthetic nonpsychoactive cannabinoid that alleviate acute pain and chronic inflammatory pain by targeting α3 GlyRs. Dehydroxylcannabidio restores the function of both hyperekplexic mutant GlyRα1 and GABAAR in the presence of GlyRα1R271Q. Apparently dehydroxylcannabidiol interrupts the protein interaction GlyRα1 and GABAAR.
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SML1679
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DEL-22379 ≥98% (HPLC)
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DEL-22379 is a cell-permeable 3-arylidene-2-oxindole derivative that inhibits the dimerization of ERK (IC50 = 500 nM) via directly binding to its dimerization interface. DEL-22379 promotes the transactivation of ELK, and prevents the EGF-induced phosphorylation of the cytoplasmic kinase RSK1 in HEK293 cells (IC50 = 500 nM). DEL-22379 induces apoptosis in various cancer cells harboring RAS-ERK pathway oncogenes (IC50 = 150 – 400 nM). DEL-22379 blocks tumor progression and metastasis in multiple xenograft models such as A375 (BRAF mutant), HCT116 (KRAS mutant) and colorectal cancer patient-derived xenografts (15 mg/kg, i.p. b.i.d.).
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SML1869
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Delafloxacin ≥98% (HPLC)
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Delafloxacin is a fluoroquinolone antibiotic active against both Gram-negative and Gram-positive bacteria such as MRSA. Delafloxacin targets both DNA gyrase and topoisomerase IV, inhibiting DNA synthesis. Unlike most fluoroquinolones, delafloxacin is weakly acidic, which increases its potency in an acidic environments such as those existing in inflammatory cells and in skin and soft tissue infections. Delafloxacin shows good activity against most fluoroquinolone-resistant strains. Delafloxacin is mostly prefered for the treatment of respiratory tract infections.
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PZ0180
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Delavirdine mesylate ≥98% (HPLC)
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Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). It is used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1.
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SML2154
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Deltarasin trihydrochloride ≥98% (HPLC)
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Deltarasin is a membrane-permeable benzimidazole derivative that effectively abolishes cellular KRas plasma membrane localization (5 μM for 1 hr) by blocking KRas-PDEδ interaction via high affinity interaction with PDEδ prenyl-binding pocket (KD = 38 nM). Deltarasin inhibits oncogenic KRas-dependent proliferation (by ~50% of Panc-Tu-I cells; 5μM for 70 hrs) and survival (52% and 46% death induction of Panc-Tu-I and Capan-1 cells, respectively; 5μM for 24 hrs) in human pancreatic ductal adenocarcinoma (PDAC) cultures and is efficacious against Panc-Tu-I xenograft-derived tumor growth in mice in vivo (60% and 80% retardation on day 9, respectively, with 15 mg/kg q.d. or 10 mg/kg b.i.d. via i.p.).
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D7696
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Demethoxycurcumin ≥98% (HPLC)
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Demethoxycurcumin (DMC) is a derivative or curcumin, and represents one of the major active components of curcumin products isolated from Curcumae sp. DMC inhibits LPS-induced nitric oxide (NO) production, and expression of iNOS and COX2 in RAW264.7 cells by blocking NF-kB activation. DMC also inhibits NF-kB dependent iNOS, TNFα and IL-1β expression in LPS-treated rat microglial cells. DMC suppresses expression of MMPs and ICAM-1 in MDA-MB-231 human breast cancer cells by inhibition of NF-kB.
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D4813
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Dendrotoxin-K ≥98% (HPLC), lyophilized powder
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Dendrotoxin-K (DTXk) is isolated from mamba snake Dendroaspis polylepis and interacts with the β-turn region in the N-terminal sequence of the potassium channel. It inhibits tumor progression in gefitinib-resistant non-small cell lung cancer cells. DTXk induces neuronal damage in the hippocampus via N-methyl-d-aspartate (NMDA) and non-NMDA receptors. Dendrotoxin-K inhibits potassium channels that contain Kv1.1 protein only.
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D7815
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R(−)-Denopamine ≥98% (HPLC), powder
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β1-adrenoceptor agonist. Denopamine is a cardiotonic drug.
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human ... ADRB1(153)
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D7000
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Deoxycorticosterone acetate
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human ... NR3C2(4306)
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P9521
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21-Deoxycortisol
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21-Deoxycortisol is a 17-hydroxyprogesterone derivative. It serves as a marker for congenital adrenal hyperplasia, an autosomal recessive disorder, indicated by 21-hydroxylase deficiency.
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D0156
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Deoxynivalenol
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D8440
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15-Deoxy-Δ12,14-prostaglandin J2 ≥95% (HPLC), 1 mg/mL in methyl acetate
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15-Deoxy-Δ12,14-prostaglandin J2 (15d-PGJ2) regulates inflammatory response in vivo. 15d-PGJ2 also elicits PPARγ-independent inhibition of nuclear factor (NF)-κB dependent transcription. It acts as an anti-angiogenic factor and triggers endothelial cell apoptosis. Selective agonist to PPARγ (peroxisome proliferator-activated receptors). Inhibits the proliferation of cancer cell lines that express PPARγ and cyclooxygenase-2 (COX-2).
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M003
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R-(−)-Deprenyl hydrochloride powder, ≥98% (HPLC)
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Selective MAO-B inhibitor; anti-Parkinsonian agent.
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human ... MAOB(4129)
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D3768
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Dequalinium chloride hydrate ≥95% (titration)
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Dequalinium chloride is a selective blocker of apamin-sensitive K+ channels and inhibitor of XIAP (X-linked inhibitor of apoptosis protein). Has been shown to induce cytotoxicity in human acute promyelocytic leukemia NB4 cells through disturbance of mitochondrial function, oxidative stress, and downregulation of Raf/MEK/ERK and PI3K/Akt signaling pathways.
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SML2014
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Deracoxib ≥98% (HPLC)
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Deracoxib is an orally active cyclooxygenase-2 (COX-2) inhibitor with >48-fold selectivity over COX-1 (IC50 of 203-189 nM against COX-2-dependent PGE2 production vs. IC50 of 9.85-9.96 μM against COX-1-dependent TxB2 production in dog whole blood). Deracoxib is also reported to exhibit inhibitory activity against phosphodiesterase (Ki = 3.6 μM against human PDE4D3) as well as positive modulatory effiacy toward 2-APB-stimulated transient receptor potential vanilloid 3 channel (TRPV3) activity.
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SML1289
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Desferrithiocin sodium salt ≥98% (HPLC)
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Desferrithiocin is an iron chelator.
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SML0649
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Deshydroxy LY-411575 ≥98% (HPLC)
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Deshydroxy LY-411575 is a cell-permeable γ-secretase inhibitor and inhibtor of Notch processing. Deshydroxy LY-411575 significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model and potently blocks Notch processing, with an IC50 of 1.7 nM in SupT1 cells. LY411575 prevents SPP (signal peptide peptidase) dependent cleavage of HCV (hepatitis C virus) core protein.
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D3900
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Desipramine hydrochloride ≥98% (TLC), powder
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Desipramine is used to treat depression. It is also used to manage enuresis in children. Desipramine helps to eliminate the pain triggered by diabetic neuropathy. Tricyclic antidepressant that is a more potent inhibitor of the norepinephrine transporter (Ki = 4 nM) than the serotonin transporter (Ki = 61 nM).
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human ... SLC6A2(6530)
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D5676
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N-Desmethylclozapine
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Major metabolite of clozapine; potent 5-HT2 serotonin receptor antagonist and a ligand for the cloned 5-HT6 and 5-HT7 serotonin receptors. Also an allosteric potentiator of M1 muscarinic receptors. N-Desmethylclozapine serves as an agonist to muscarinic acetylcholine receptors, and is known to exert its antipsychotic action. It blocks synaptic transmission by antagonizing synaptic GABA (γ-aminobutyric acid) receptors.
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human ... KCNH1(3756)
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UC305
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O-Desmethylnaproxen
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CYP2C9 metabolite of naproxen
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D204
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S-(+)-O-Desmethylraclopride hydrobromide solid, ≥98% (HPLC)
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D9069
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N-Desmethyltamoxifen HCl ≥98% (HPLC), solid
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N-Desmethyltamoxifen HCl is the primary metabolite of tamoxifen. N-Desmethyltamoxifen HCl is an estrogen response modifer and protein kinase C inhibitor.
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UC304
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O-Desmethyltramadol
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O-Desmethyltramadol has a high affinity towards opioid receptors and is responsible for the analgesic effect of the μ-opioid receptor Metabolite of tramadol
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D6513
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Desmosterol ≥84% (GC)
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D2069
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Desvenlafaxine hydrochloride ≥98% (HPLC), powder
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Desvenlafaxine hydrochloride is a dual SERT/NET reuptake inhibitor. It is a major active metabolite of venlafaxine (#542); brain penetrant; Ki = 40 nM and 122 nM for hSERT and hNET, respectively (weak binding at the hDAT). Inhibition of [3H]5-HT or [3H]NE uptake for the hSERT or hNET produced IC50 values of 47 and 531 nM. Desvenlafaxine hydrochloride is a psychoactive drug. Incidence of this drug in environmental samples might induce in vitro gene expression associated with neurological disorders.
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D3821
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Devazepide ≥98% (HPLC), powder
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Devazepide is a CCK1 (CCK-A) receptor antagonist and a CCK8 antagonist. Devazepide is a cholecystokinin octapeptide (CCK1) (CCK-A) receptor antagonist. It inhibits CCK binding to peripheral-type receptor (CCK-A). Devazepide reverses the cholecystokinin octapeptide (CCK-8) based antagonism towards morphine.
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D1756
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Dexamethasone ≥98% (HPLC), powder
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Dexamethasone is known to be effective against relapsed multiple myeloma. It is found to decrease inflammation associated with cerebrospinal fluid and central nervous system (CNS) complications, such as hearing loss. Glucocorticoid anti-inflammatory agent. Regulates T cell survival, growth, and differentiation. Inhibits the induction of nitric oxide synthase.
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human ... ABCB1(5243), CYP3A4(1576), IL4(3565), IL5(3567), NR3C1(2908) mouse ... Abcb1a(18671), Abcb1b(18669), Ifng(15978), Nos2(18126), Ptgs2(19225), Tnf(21926) rat ... Ar(24208), Nr3c1(24413), Tnf(24835)
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D1881
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Dexamethasone 21-acetate ≥99%
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Dexamethasone 21-acetate or dexamethasone acetate is a derivative of dexamethasone. It is a hydrophobic drug. Dexamethasone is a glucocorticoid possessing anti-inflammatory activity.
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human ... NR3C1(2908)
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SML2624
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Dexlansoprazole ≥98% (HPLC)
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Dexlansoprazole is a proton pump inhibitor. It is the active enantiomer of lansoprazole used to treat gastroesophageal reflux disease (GERD).
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SML0956
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Dexmedetomidine hydrochloride ≥98% (HPLC)
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Dexmedetomidine hydrochloride is a highly potent and selective α2-adrenergic agonist with analgesic and sedative properties, the (+)-isomer of medetomidine. Dexmedetomidine hydrochloride is used clinically as an anesthetic agent to reduce anxiety and tension and promote relaxation and sedation without causing respiratory depression.
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SML0392
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Dexpramipexole dihydrochloride ≥98% (HPLC)
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R-(+)-Pramipexole is a neuroprotective agent; weak non-ergoline dopamine agonist. R-(+)-Pramipexole has been found to have neuroprotective effects and is being investigated for treatment of ALS. It reduces mitochondrial reactive oxygen species (ROS) production, inhibits the activation of apoptotic pathways, and increase cell survival in response to a variety of neurotoxins and β-amyloid neurotoxicity. Compared to the S-(-) isomer, R-(+)-Pramipexole has much lower dopamine agonist activity.
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D1446
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Dexrazoxane ≥95% (HPLC)
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Dexrazoxane is a cardioprotective compound against anthracyclines. It functions by inhibiting topoisomerase II without inducing DNA strand breaks. Dexrazoxane is a + enantiomer of razoxane.
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D2531
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Dextromethorphan hydrobromide monohydrate ≥99% (TLC)
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Dextromethorphan hydrobromide is an allosteric antagonist at N-methyl D- aspartate (NMDA)-controlled ion channels and antagonist at voltage-dependent channels. Dextromethorphan hydrobromide is useful in treating dry cough.
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human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRIN3A(116443), GRIN3B(116444), SIGMAR1(10280)
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UC205
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Dextrorphan
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human ... GRIN2A(2903) rat ... Grin2a(24409)
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SML1627
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DFHBI
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3,5-difluoro-4-hydroxybenzylidene imidazolinone (DFHBI) is non fluorescent when unbound. DFHBI is a membrane permeable and nontoxic fluorogen, which produces fluorescence upon binding. RNA aptamers Spinach, Spinach2 and Broccoli. DFHBI displays fluorescence excitation maxima of 447 nm and peak fluorescence emission of 501 nm. DFHBI is used for imaging RNA in cells.
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SML2697
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DFHBI-1T ≥98% (HPLC)
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DFHBI-IT is a membrane-permeable, non-cytotoxic, RNA aptamers-activated fluorescence probe widely employed in varous detection systems utilizing compatible RNA tags such as Spinach, Spinach2, iSpinach, and Broccoli. Upon binding Spinach2, DFHBI-1T offers brighter fluorescence than DFHBI due to increased extinction coefficient & quantum yield (by 1.4- and 1.3-fold, respectively). DFHBI-1T is also better suited for devices optimized for GFP or fluorescein detection/imaging due to its red shift in excitation & emission wavelengths (Spinach2-comlex Ex/Em = 482/505 nm with DFHBI-1T vs 447/501 nm with DFHBI).
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SML0994
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DFU ≥98% (HPLC)
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DFU is an orally available highly selective cyclo-oxygenase-2 (COX-2) inhibitor that potently inhibits lipopolysaccharide (LPS)-induced PGE2 production in a human whole blood assay.
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SML1642
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DHED ≥98% (HPLC)
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DHED (10β,17β-dihydroxyestra-1,4-dien-3-one) is an inactive prodrug that selectively produces estrogen solely in the brain. DHED is converted to 17β-estradiol in the brain by an enzyme only expressed in the CNS, but is inert in the rest of the body. DHED was found to provide neuroprotection in a rat stroke model and reversed neurological symptoms of estrogen deprivation such as memory problems in female rats lacking ovaries. DHED is a substrate for nicotinamide adenine dinucleotide phosphate (NADPH)-dependent dehydrogenase/reductase. Its expression in the brain is correlated to neuroprotection functionality.
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D5919
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Diacylglycerol Kinase Inhibitor I solid
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Diacylglycerol kinase inhibitor. Inhibits formation of [38P]1-Oleoxyl-2-acetylglyceryl-3-phosphoric acid (OAPA) in red blood cell membranes: IC50 = 3.3 μM.
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D5794
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Diacylglycerol Kinase Inhibitor II solid
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Diacylglycerol kinase inhibitor. Inhibits formation of [38P]1-Oleoyl-2-acetylglyceryl-3-phosphoric acid (OAPA) in red blood cell membranes: IC50 = 3.3 μM.
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P7769
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1,2-Diacyl-sn-glycero-3-phospho-L-serine ≥97% (TLC), from bovine brain, amorphous powder
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1,2-Diacyl-sn-glycero-3-phospho-L-serine or phosphatidylserine (PS) is a structurally diverse acidic phospholipid having fatty acid ester at the glycerol sn positions. Bovine brain cortex based PS is a potent brain nutrient. It favors neurotransmission and may improve memory in dementia. PS is also the major membrane phospholipid associated with the nuclear membrane, myelin, endoplasmic reticulum, Golgi and mitochondria. The synthesis of PS is catalyzed by phosphatidylserine synthase 1 from L-serine and CDP-diacylglycerol in the mitochondria-associated membrane (MAM) domains of the endoplasmic reticulum. PS is externalized during phagocytosis and is dysregulated in tumors making it a potential marker for therapeutic targeting. A slowly metabolized structural phospholipid found mainly in gray matter.
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D1262
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P1,P4-Di(adenosine-5′) tetraphosphate ammonium salt ≥95% (HPLC), powder
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Diadenosine polyphosphate (Ap4A) functions as a second messenger in pancreatic cells. Diadenosine polyphosphate is majorly stored in neuronal cells, thrombocytes and chromaffin. It stimulates phospholipase D, fluctuates intracellular calcium levels, induces nitric oxide release, activates 5′-nucleotidase, and inhibits adenosine kinase activity in vitro. The membrane-bound ectoenzymes in endothelial cells in blood plasma and smooth muscle cell metabolize Ap4A.
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human ... PLD1(5337), PLD2(5338), PLD3(23646), PLD4(122618), PLD5(200150)
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P4394
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cis-Diammineplatinum(II) dichloride crystalline
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Potent chemoimmunotherapeutic drug; stimulates the immune responses by activating macrophages and other cells of the immune system. Cisplatin-treated macrophages show increased antigen presentation function in vitro. Treatment increased cellular NF-κB content and translocation in macrophages. Cisplatin effects are regulated by kinases, phosphatases, and Ca2+/calmodulin. Forms cytotoxic adducts with the DNA dinucleotide d(pGpG), inducing intrastrand crosslinks. Potent platinum-based antineoplastic agent. Forms cytotoxic adducts with the DNA dinucleotide d(pGpG), inducing intrastrand cross-links.
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SML0927
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Diapocynin ≥98% (HPLC)
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Diapocynin is a covalent dimer of apocynin, and a functional metabolite of the same. It is generated by neutrophil activation via myeloperoxidase-mediated oxidation. Studies show that diapocynin has greater neuroprotection compared to apocynin. Diapocynin, a proposed NADPH oxidase (NOX) inhibitor, is an anti-inflammatory and antioxidant agent. Diapocynin attenuates oxidative damage and neuroinflammatory responses in animal model of Parkinson’s disease. Diapocynin reverses deficient motor coordination in LRRK2R1441Gtg mice of PD.
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SML2337
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Diasarone-I ≥98% (HPLC)
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Diasarone-I is an antiviral agent isolated form Acorus tatarinowii Schott that potently inhibits dengue viral infection. Diasarone-I is binds to the viral 2′O methyltransferase of nonstructural protein 5 (NS5). It also decreases the DENV2-induced STAT1 phosphorylation and IFN-stimulated genes (ISGs) expression. The antiviral effect of Diasarone-I includes half maximal effective concentration (EC50) of 4.5 μM and half maximal cytotoxicity concentration (CC50) of >80 μM.
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D0899
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Diazepam
|
Diazepam is a benzodiazepine anxiolytic agent. It serves as a prototype ligand for the GABAA receptor benzodiazepine modulatory site. Diazepam is often used as a sedative. Its metabolism involves cytochrome P450 (CYP) 2C19 and 3A4. Diazepam has immediate action upon administration.
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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) rat ... Gabra1(29705), Gabra2(29706)
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D9035
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Diazoxide
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Selective ATP-sensitive K+ channel activator in both vascular smooth muscle and pancreatic β-cells; antihypertensive.
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human ... KCNA1(3736), KCNJ11(3767), KCNJ8(3764), KCNMA1(3778) mouse ... Kcnj1(56379), Kcnj11(16514) rat ... Gria1(50592), Kcna1(24520), Kcnj1(24521), Kcnj11(83535), Kcnj8(25472)
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W0641
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W-84 dibromide ≥98% (HPLC), solid
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Potent allosteric modulator of M2 muscarinic acetylcholine receptors.
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D0260
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N6,2′-O-Dibutyryladenosine 3′,5′-cyclic monophosphate sodium salt ≥97% (HPLC), powder
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Cell-permeable cAMP analog that activates cAMP dependent protein kinase (PKA).
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D8190
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3′,4′-Dichlorobenzamil hydrochloride >98% (HPLC)
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Inhibits Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels.
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D1916
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5,6-Dichlorobenzimidazole 1-β-D-ribofuranoside
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5,6-Dichlorobenzimidazole 1-β-D-ribofuranoside (DRB), a nucleoside analog that halts mRNA synthesis by phosphorylation of the C-terminal domain of RNA polymerase II, making it inactive. It also interferes with the DNA topoisomerase II, may modulate response to cytokines and blocks the human immunodeficiency virus (HIV) via RNA modification. It also inhibits cyclin-dependent kinases (CDKs) 7 and 9 and favors apoptosis in leukemic cells. It may serve as a therapeutic agent in treating cancer. Inhibitor of RNA synthesis; causes premature termination of transcription. CK2 (casein kinase-2) inhibitor.
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human ... CSNK2A1(1457), CSNK2B(1460)
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D6883
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2′,7′-Dichlorofluorescin diacetate ≥97%
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D4434
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Dichloromethylenediphosphonic acid disodium salt
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Analog of pyrophosphate ion that inhibits the osteoclastic activity leading to bone resorption and osteoporosis. The compound is used in cancer research, especially in skeletal metastases and breast carcinoma. When entrapped in liposomes, it is used for macrophage-selective depletion (macrophage "suicide" technique), especially in spleen and liver. Found also to inhibit collagenase and matrix metalloproteinase1.
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rat ... Man2a1(25478), Si(497756)
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D6899
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Diclofenac sodium salt
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Diclofenac sodium salt is a nonsteroidal anti-inflammatory drug (NSAID) that acts as a competitive and irreversible inhibitor of prostaglandin synthetase. Its analgesic and anti-inflammatory activities are based on the prevention of the synthesis of arachinodate metabolites via cyclooxygenase inhibition. It is found to hinder the conversion of arachidonic acid to prostaglandins, which mediate inflammatory process. The NSAIDs are found to inhibit both cyclooxygenase enzymes, COX-1 and COX-2, causing undesirable gastrointestinal effect. Diclofenac sodium also functions as a scavenger of free radicals and serves a radioprotective role in restoring supercoiled form of plasmid DNA damaged by radiation back to normal. Diclofenac sodium is oxidized by the donation of electron and transfer of hydrogen atom. It can be a potential radioprotective agent. Standard NSAID and cyclooxygenase (COX) inhibitor. Major metabolites are 4´-hydroxydiclofenac and 5´-hydroxydiclofenac. Has been used as substrate selective for CYP2C9.
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human ... PTGS1(5742), PTGS2(5743)
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D7909
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Dicyclomine hydrochloride ≥99% (TLC), powder
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Competitive muscarinic acetylcholine receptor antagonist.
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human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
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D1413
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2′,3′-Didehydro-3′-deoxythymidine ≥98% (TLC)
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2′,3′-Didehydro-3′-deoxythymidine is a nucleoside analog, which inhibits HIV replication in vitro. Stavudine has the ability to enter the cells by non-facilitated diffusion. It possesses inhibitory activity against moloney murine leukemia virus, friend murine leukemia virus and simian immunodeficiency virus.
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D7408
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2′,5′-Dideoxyadenosine ≥95% (HPLC), solid
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Cell-permeable adenylyl cyclase inhibitor. IC50 = 2.7 μM in detergent-dispersed rat brain preparations.
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rat ... Adcy2(81636)
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D8174
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9,11-Dideoxy-11α,9α-epoxymethanoprostaglandin F2α solution, 10 mg/mL in methyl acetate
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Thromboxane receptor agonist.
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D0400
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9,11-Dideoxy-9α,11α-epoxymethanoprostaglandin F2α
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Prostaglandin F2α analogue; thromboxane A2/prostaglandin H2 mimetic.
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D3658
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1,9-Dideoxyforskolin from Coleus forskohlii ≥97%, solid
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Biologically inactive forskolin analog. Does not stimulate adenylyl cyclase.
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SML2035
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Didox ≥98% (HPLC)
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Didox is a ribonucleotide reductase (RNR) inhibitor that inhibits proliferation of and decreased secretion of cytokines IL-6, IFN-g, TNF-a, IL-2, IL-13, IL-10 and IL-4. Didox inhibits proliferation of tamoxifen-resistant breast cancer cells. Didox is an antioxidant that potentiates the cytotoxic profile of doxorubicin.
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SML1468
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Dienogest ≥98% (HPLC)
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Dienogest is a fourth-generation progestin, an orally active synthetic progestogen with approximately 10% of the relative affinity of progesterone, but has a very potent progestagenic effect in the endometrium with some antiandrogenic activity and without any androgenic, glucocorticoid or mineralocorticoid effects. It has been used alone or in combination as a contraceptive and to treat uterine fibroids. Dienogest inhibits ovulation primarily through peripheral action rather than by central action on gonadotrophin secretion. Dienogest is used to treat endometriosis. It might also help to decrease the levels of plasma estradiol by stimulating cell death of granulosa cells in the ovary.
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D184
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Diethylamine NONOate sodium salt hydrate ≥97% (NMR)
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Diethylamine NONOate is a complex of diethylamine with nitric oxide used to generate a controlled release of nitric oxide in solution.
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D185
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Diethylenetriamine/nitric oxide adduct ≥97% (NMR), solid
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Diethylenetriamine/nitric oxide adduct (DETA/NO) is a NONOate, which has the longest NO?generating half?life in vitro. Inhaled DETA/NO acts as a pulmonary vasodilator in animals and humans. This NO donor releases nitric oxide in solution in a controlled manner. DETA/NO is associated with protein downregulation, upregulation of p53 expression. It enhances p53 post-translational modifications and also downregulates Nanog and Oct4 mRNA.
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D4628
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Diethylstilbestrol ≥99% (HPLC)
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Diethylstilbestrol is a synthetic estrogen with carcinogenic properties. Causes renal clear-cell carcinoma in Syrian hamster. In humans it causes increased risk of breast cancer, clear cell adenocarcinoma (CCA) of the vagina and cervix, and reproductive anomalies. Used in the treatment of prostate cancer to block the production of testosterone.
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human ... ESR1(2099), ESR2(2100), ESRRG(2104) mouse ... Esr1(13982) rat ... Ar(24208), Esr1(24890)
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D7692
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Diethylumbelliferyl phosphate ≥98% (HPLC), oil
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Diethylumbelliferyl phosphate (DEUP), an organophosphate does not block protein kinase activity A in vitro. Diethylumbelliferyl phosphate is a selective, potent cholesterol esterase inhibitor. It blocks steroidogenesis primarily by preventing cholesterol transport into the mitochondria of steroidogenic cells. Inhibitors of cholesterol esterase are anticipated to limit the absorption of dietary cholesterol. IC50 = 11.6 μM.
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SML0599
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DIF-1 ≥98% (HPLC)
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DIF-1 (differentiation-inducing factor-1) is isolated from a Dictyostelium slime mold, and is used to inhibit proliferation/promote differentiation in various cell lines. DIF-1 is a cell differentiation inducing factor. Differentiation-inducing factor-1 (DIF-1) blocks the migration and invasion of cells and decreases the expression of matrix metalloproteinase-2. It prevents the proliferation of cells using glycogen synthase kinase-3 (GSK-3)-dependent mechanism. DIF-1 is more active when compared to DIF-2 in promoting stalk cell differentiation under submerged assay conditions.
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D0567
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DIF-3 ≥99% (HPLC), solid
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DIF-3 Inhibits cell cycle by inducing G0/G1 arrest.
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SML2666
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Diflapolin ≥98% (HPLC)
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Diflapolin is a bioavailable, highly potent and highly selective dual FLAP/sEH (5-LO-activating protein/ soluble epoxide hydrolase) inhibitor that suppresses leukotriene formation and increases epoxyeicosatrienoic acids levels. Diflapolin exhibit potent anti-inflammatory activities in mice models.
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D193
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DL-α-Difluoromethylornithine hydrochloride hydrate solid, ≥97% (NMR)
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Difluoromethylornithine (Eflornithine) inhibits polyamine biosynthesis by the selective, irreversible inhibition of ornithine decarboxylase (ODC). A chemoprotective agent that blocks angiogenesis.
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human ... ODC1(4953)
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D8941
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2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide ≥98% (HPLC), solid
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2,6-Difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor agonist that reduces ischemia-induced performance deficits in rats.
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human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
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D6288
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6α,9α-Difluoroprednisolone 21-acetate 17-butyrate ≥98%
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human ... NR3C1(2908)
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SML1976
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DIM-C-pPhCO2Me ≥98% (HPLC)
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DIM-C-pPhCO2Me is a NR4A1 (Nur77) antagonist that exhibit potent anticancer activity in pancreatic, colon, breast, kidney, and rhabdomyosarcoma cells. DIM-C-pPhCO2Me decreases expression of PAX3-FOXO1A and β1-integrin proteins in Rh30 rhabdomyosarcoma and MDA-MB-231 breast cancer cells. DIM-C-pPhCO2Me inhibits migration of Rh30 and MDA-MB-231 cancer cells. DIM-C-pPhCO2Me is also known as 1,1-bis(3′-indolyl)-1-(p-carboxymethylphenyl)methane. In pancreatic and colon cancer cells, DIM-C-pPhCO2Me plays an inhibitory role on cell migration. DIM-C-pPhCO2Me prevents the action of mechanistic target of rapamycin (mTOR) and reduces the multiplication and survival of cancer cells. It stimulates reactive oxygen species (ROS) in various cancer cell lines.
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SML1220
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Doripenem hydrate ≥98% (HPLC)
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Doripenem hydrate is used to treat complicated urinary infection including Pyelonephritis caused by E.coli. Doripenem hydrate is promoted in the United States as DORIBAX®. This drug is synthesized from p-nitrobenzyl-protected enolphosphate 2b and N-(p-nitrobenzyloxycarbonyl)-protected aminomethylpyrrolidine. Doripenem is an ultra-broad spectrum carbopenem antibiotic. Doripenem is active against both gram-positive and gram-negative bacteria.
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SML2496
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D-I03 ≥98% (HPLC)
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D-I03 is a selective RAD52 inhibitor (IC50 = 5 and 8 μM, respectively, by SSA and DNA pairing (D-loop formation) assay; <5% RAD51 inhibition at 80 μM) that blocks single-strand DNA (ssDNA) annealing (SSA)-, but not homology dependent recombination (HDR)-, mediated double-strand break (DSB) repair (5-30 μM using respective U2OS reporter cells) and reduces nuclear RAD52, but not RAD51, foci formation (2.5 μM) upon DNA damage by cisplatin. D-I03 selectively suppresses BRCA1-deficient over BRCA1-proficient cancer cells and exerts synergistic activity with PARP1 inhibitors against BRCA1-deficient cancer both in cultures (1 & 2.5 μM) and in mice (50 mg/kg/day i.p.) in vivo.
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SML2191
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D-Moses ≥98% (HPLC)
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D-Moses is a negative control to L-Moses a cell penetrant, potent and selective PCAF bromodomain (Brd) inhibitor.
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SML2358
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D-NMAPPD ≥98% (HPLC)
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D-NMAPPD (B13), a myristoyl-CoA analog, is a cell penetrant inhibitor of N-myristoyltransferases that suppressed FRS2α (fibroblast growth factor receptor substrate 2) myristoylation. D-NMAPPD inhibits wild-type FGFRs and drug-resistant mutants (FGFRsDRM) oncogenic signaling in cancer cells. D-NMAPPD potently inhibits growth of xenograft tumors in mice. D-NMAPPD is a potent inhibitor of ceramidase that elevates endogenous ceramide levels and suppress growth of cancer cells.
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