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SML1687 3BDO ≥98% (HPLC) 3BDO is a cell-permeable, orally bioavailable, non-toxic butyrolactone derivative that is shown to competitively bind FKBP1A (FK506-binding protein 1A, 12 kDa) in a reversible manner, and suppress autophagy via the mTOR pathway. 3BDO inhibits both LPS- and oxLDL-induced autophagy in HUVECs, increases TIA1 phosphorylation, and reduces autophagosomes number. It is reported to be brain permeant, and significantly decreases atherosclerosis development in apoE-/- mice (100 mg/kg, q.d., p.o.). 3BDO increases IDE and neprilysin levels, lowers amyloid-β deposition in an AβPP/PS1 transgenic mouse model of Alzheimer′s disease, and alleviates memory deficits.
 
SML1167 4BP-TQS ≥98% (HPLC) 4BP-TQS is an atypical agonist of a7-nAChR that binds to the receptor in an intrasubunit cavity, and activates the channel via a mechanism that is distinct from conventional agonists. Maximal activation of a7-nAChR by 4BP-TQS is eight fold greater than activation by a maximum dose of acetylcholine (Ach), and 4BP-TQS can poteniate an EC10 concentration of ACh to invoke a response that is 540-fold higher than the maximal dose of ACh alone.
 
SML1419 B32B3 ≥95% (HPLC) B32B3 is a potent, selective and cell permeable VprBP inhibitor that suppresses xenograft tumor growth. B32B3 potently inhibits VprBP dependent formation of phosphorylated histone H2A on threonine 120 (H2AT120p).
 
B7438 6-B345TTQ >98% (HPLC) 6-B345TTQ is a non-cytotoxic inhibitor of α4 integrin paxillin interaction.
 
SML1007   B355252 ≥98% (HPLC) B355252 is a neuroprotective agent that potentiates nerve growth factor (NGF)-induced neurite outgrowth and protects against cell death caused by glutamate-evoked oxidative stress. In a murine hippocampal neuronal cell line, B355252 increased cell viability and protected against cell death caused by glutamate-induced toxicity, inhibiting glutamate-evoked increase in intracellular Ca2+ and ROS production.
 
B2559 B581 >95% (HPLC), solid Stable and membrane permeable inhibitor of farnesyltransferase.
rat ... Fnta(25318)
SML0102   Bac2A trifluoroacetate salt ≥98% (HPLC) Bac2A is an antimicrobial and immunomodulatory peptide. Bac2A is a linear variant of bactenecin. Recent studies show that Bac2A is very effective against fungal pathogens, Fusarium oxysporum f. sp. vasinfectum and Fusarium graminearum. In these studies, Bac2A antifungal activity was not due to membrane destabilization but rather to interaction with intracellular targets.
 
B1793 Bafilomycin A1 from Streptomyces griseus ≥90% (HPLC) A specific inhibitor of vacuolar type H+-ATPase (V-ATPase) in animal cells, plant cells and microorganisms.
 
SML1760 BAM15 ≥98% (HPLC) New BAM15 is a cell penetrant and potent uncoupler of oxidative phosphorylation in mitochondria that that does not depolarizes the plasma membrane. BAM15 protects mice from acute renal ischemic-reperfusion injury.
 
SML0641   BAM7 ≥98% (HPLC) BAM7 is a selective activator of BAX, a proapoptotic member of the BCL-2 protein family. BAM7 binds directly to the BAX trigger site, a distinct BH3 binding site that regulates BAX activation, inducing BAX oligomerization, which enables the release of apoptogenic factors that result in cell death. BAM7 is selective for this previously unknown BH3-binding groove on the N-terminal face of BAX.
 
SML0729   BAM8-22 trifluoroacetate salt ≥98% (HPLC) BAM8-22 is a selective agonist for the sensory neuron specific G-protein coupled receptors (SNSRs). BAM8-22 inhibits development of morphine tolerance in rats. BAM8-22 is inactive at opioid receptors. Also, BAM8–22 is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM8-22 produces itch and nociceptive sensations in humans in a histamine-independent manner.
 
B8684 Bambuterol hydrochloride >98% (HPLC), powder β-adrenoceptor agonist; bronchodilator; anti-asthmatic; terbutaline prodrug
 
SML1854 Banoxantrone dihydrochloride ≥98% (HPLC) Banoxantrone (AQ4N) is a hypoxia-activated prodrug of topoisomerase II inhibitor AQ4 (Bioreductive AQ4 precursor).
 
SML0979 Bantag-1 trifluoroacetate salt ≥95% (HPLC) Bantag-1 is a very specific, high affinity antagonist of the orphan GPCR Bombesin receptor subtype-3 (BRS-3). The binding affinity of Bantag-1 in BRS-3 expressing cells is 1.3 nM.
 
A1076 BAPTA-AM ≥95% (HPLC) Selective chelator of intracellular Ca2+ stores.
 
B4061 BATCP ≥98% (HPLC), solid HDAC 6 selective substrate (over HDAC 1, Class II over Class I).
 
SML0041 Batimastat ≥98% (HPLC) Batimastat is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor.
Batimastat is hydroxamate-type inhibitor of matrix metalloproteinases (MMP). It inhibits the growth and spread of lung tumors, breast cancer regrowth and human colon tumor growth and spread in mouse models. Batimastat reduces MMP-mediated vascular dysfunction and vessel wall damage and enhances the sealing ability and bond strength of dental adhesives.
 
SML0411 BAY-X-1005 ≥98% (HPLC) Bay-X-1005 is a potent inhibitor of 5-lipoxygenase activating protein (FLAP). Bay-X-1005 inhibits A23187-induced LTB4 production in human leucocytes with an IC50 value of 220 nM, and blocks IgE mediated airway contractions.
 
B5556 Bay 11-7082 ≥98% (HPLC), powder Bay 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation.
 
B5681 Bay 11-7085 ≥98% (HPLC), solid Inhibits NF-κB activated expression of ICAM-1, VCAM-1, E-selectin, IL-6 and IL-8.
human ... NFKB1(4790)
B8810 BAY 41-2272 ≥97% (HPLC) BAY 41-2272 is an activator of soluble guanylate cyclase at a novel, NO-independent regulatory site. BAY 41-2272 is the first product that stimulates sGC through a non-NO mechanism. BAY 41-2272 inhibits platelet aggregation and induces vasorelaxation without nitrate tolerance.
 
SML1756 BAY-299 ≥98% (HPLC) BAY-299 is a potent and selective inhibitor of BRD1 and the second bromodomain of TAF1 (Transcription initiation factor TFIID subunits 1). BAY-299 is selective over other bromodomains including the other members of the BRPF family, and BRD9, ATAD2 and BRD4. BAY-364 is structurally similar to BAY-299 and serves as inactive control. For full characterization details, please visit the BAY-299 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1783 BAY-299N ≥98% (HPLC) BAY-299N (BAY-364) is structurally similar to selective BRD1/TAF1 inhibitor BAY-299 and serves as inactive control. BAY-299N is inactive against BRD1 and exhibit moderate activity against TAF1 (3 μM).
 
B9685 BAY 61-3606 hydrochloride hydrate ≥98% (HPLC), powder Spleen tyrosine kinase (Syk) inhibitor; anti-inflammatory. Syk plays a major role in inflammation pathways via receptors for the Fc portion of immunoglobulins, as well as B cell signaling. It is orally active, potent (Ki 7.5 nM), and highly selective for Syk vs other kinases (Lyn, Fyn, Src, Itk, Btk; Ki′s).
 
SML1780 BAY-588 ≥98% (HPLC) BAY-588 is an inactive control probe for BAY-876 (catalog no. SML1774). BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. For characterization details of BAY-876 and BAY-588, please visit the BAY-876 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
 
SML1603 BAY-598 ≥98% (HPLC) BAY-598 is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), a lysine methyl transferase inhibitor that dimethylates histone H3K36 and methylates histone H3K4. SMYD2 also methylates Lys-370 of p53, leading to decreased DNA-binding activity. SMYD2 is over-expressed in several cancers with poor prognosis. BAY-598 inhibits in vitro methylation of p53K370 with an IC50 value of 27 nM and in cells with an IC50 value < 1 μM. BAY-598 is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. BAY-598 can be used with in vivo experiments. For full characterization details, please visit the BAY-598 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
B3561 BAY 73-6691 ≥98% (HPLC), powder BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. This compound selectively inhibits human (IC50 = 55 nM) and murine (IC50 = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.†
 
SML1564 BAY-677 ≥98% (HPLC) BAY-677 is the negative control probe for BAY-678 (catalog no. SML1563), which is a human neutrophil elastase (HNE) inhibitor with >2,000-fold selectivity for HNE over a panel of 21 other serine proteases. For characterization details of BAY-678 and BAY-677, please visit the BAY-677 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
 
SML1563 BAY-678 ≥98% (HPLC) BAY-678 is an orally available, highly potent and selective inhibitor of human neutrophil elastase (HNE). For full characterization details, please visit the BAY-678 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
 
SML1774 BAY-876 ≥98% (HPLC) BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins. For full characterization details, please visit the BAY-876 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
 
B133 (S)-(−)-Bay K8644 ≥98% (HPLC), solid Ca2+ channel activator; enantiomer of Bay K 8644.
human ... ADORA3(140)
rat ... Adora1(29290), Adora2a(25369)
B3936 BAY R3401 ≥98% (HPLC), solid BAY R3401 is a glycogen phosphorylase inhibitor. The racemic prodrug, BAY R3401, suppresses hepatic glycogenolysis. BAY W1807, the active metabolite of BAY R3401, inhibits muscle glycogen phosphorylase a and b. It has been investigated that the metabolites of BAY R3401 suppress hepatic glycogenolysis by allosteric inhibition and dephosphorylation of phosphorylase a.
 
B3686 BAY U6751 hydrate solid, ≥98% (HPLC) BAY W1807, the active metabolite of BAY R3401, inhibits muscle glycogen phosphorylase a and b. In gel-filtered liver extracts, racemic BAY U6751 (containing active BAY W1807) was tested for inhibition of phosphorylase in the glycogenolytic (in which only phosphorylase a is active). In liver extracts, BAY U6751 (0.9-36 μmol/L) inhibited glycogen synthesis by phosphorylase b (notwithstanding the inclusion of AMP), but not by phosphorylase a. Inhibition of phosphorylase-a-catalyzed glycogenolysis was partially relieved by AMP (500 μmol/L). BAY U6751 facilitated phosphorylase-a dephosphorylation. Isolated hepatocytes and perfused livers were tested for BAY R3401-induced changes in phosphorylase-a:b ratios and glycogenolytic output.
 
B9680 Bay u9773 ≥98% (HPLC), oil Subtype-selective cysteinyl-leukotriene (Cys-Lt) antagonist.
 
SML1276 BAZ2-ICR ≥98% (HPLC) BAZ2-ICR is a chemical probe for BAZ2A/B bromodomains with >100-fold selectivity over other bromodomains, with the exception of CECR2 (15-fold selectivity). BAZ2A is an essential component of the nucleolar remodeling complex (NoRC), which mediates recruitment of histone modifyine enzymes and DNA methylase involved in the silencing of ribosomal RNA transcription by RNA polymerase I. BAZ2B is believed to be involved in regulating nucleosome mobilization along linear DNA. BAZ2-ICR binds to BAZ2A with a KD of 109 nM (ITC) and to BAZ2B with a KD of 170 nM (ITC). BAZ2-ICR also shows accelerated Fluorescence recovery after photobleaching (FRAP) recovery at 1 μM in the BAZ2A FRAP assay. For full characterization details, please visit the BAZ2-ICR probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
PZ0018   Bazedoxifene acetate ≥98% (HPLC) Bazedoxifene is a third generation nonsteroidal selective estrogen receptor modulator (SERM), used clinically to treat postmenopausal osteoporosis. Bazedoxifene binds to estrogen receptor-α with IC50 = 26 nM, similar to that of raloxifene, but lower affinity than 17-β estradiol. Bazedoxifene did not stimulate proliferation of MCF-7 cells, instead inhibited 17β -estradiol-induced proliferation with IC50 = 0.19 nM, exhibiting a desirable profile of agonist/antagonist activity.
 
SML1049   BC-1215 ≥98% (HPLC) BC-1215 is a Fbxo3 ubiquitin E3 ligase activity inhibitor that reduces severity of cytokine-driven inflammation in several mouse disease models. BC-1215 decreased Fbxo3-Fbxl2 interaction and prevented SCF-Fbxo3–catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6.
 
SML1021 BC-1258 BC-1258 is a potent activator of unique E3 ligase F-box/LRR-repeat protein 2 (FBXL2) that increases levels of FBXLs protein, thus promoting Aurora B degradation. BC-1258 induces mitotic arrest and apoptosis of tumorigenic cells. Also BC-1258 inhibits tumor formation in athymic nude mice.
 
SML1097 BC8-15 ≥98% (HPLC) BC8-15 is a potent PDE4/8 inhibitor that elevates steroidogenesis in mouse Leydig cells.
 
SML1817   BCI-121 ≥98% (HPLC) BCI-121 is a substrate-competitive SMYD3 inhibitor that reduces nuclear histone H3 lys4 di- and tri-methylation level (by 50%/H3K4me2 and 40%H3K4me3 in HT29 cells; 100 μM BCI-121 for 48 h), downregulates known SMYD3 target genes transcription, and selectively affects SMYD3-dependent proliferation of cancer cultures (46%/HT29 and 54%/HCT116 proliferation reduction; 100 μM BCI-121 for 72 h) with little antiproliferation efficacy toward low SMYD3-expressing cancer cells. BCI-121 targets SMYD3 via direct affinity interaction (kon 357.7/M/s; koff 4.23×10-3/s; KD=koff/kon = 11.8 μM) and effectively competes against histone for SMYD3 binding (%inhibition/[histone H4 peptide]:[BCI-121] ratio = 36.5%/1:1 and 51.0%/1:2.5).
 
B4313 (E/Z)-BCI hydrochloride ≥98% (HPLC) BCI is an allosteric inhibitor of Dusp6 that acts within the phosphatase domain to prevent the catalytic stimulation of phosphatase activity induced by ERK2 substrate binding. BCI also hyperactivates FGF signaling, since Dusp6 functions as a feedback regulator of FGF signaling.
 
SML0355 BCTC ≥98% (HPLC) BCTC is a potent antagonist of the vanilloid receptor TRPV1. BCTC blocks capsaicin-induced contractions in a variety of smooth muscle tissues, including guinea pig ileum, bladder and trachea with no effects on capsaicin-sensitive, sensory neuron-mediated positive inotropy. The compound penetrates the CNS and has strong analgesic properties.
 
B8562 BD 1047 dihydrobromide ≥95% (HPLC) BD-1047 is a selective, putative σ receptor antagonist with antidystonic activity. BD-1047 has >50-fold selectivity at σ1 over σ2 and also >100-fold selectivity over opiate, phencyclidine, muscarinic, dopamine, α1- & α2-adrenoceptor, 5-HT1, and 5-HT2. Though s receptor antagonism is consistent with antipsychotic, especially anti-schizophrenic, activity, BD-1047 shows only modest activity in animal screens for antipsychotics.
 
SML0276 BD 1063 dihydrochloride ≥98% (HPLC) BD 1063 is a potent sigma(1) receptor antagonist; approximately 50-fold selective for sigma-1 over sigma-2 and 100-fold or more selective over 9 other tested neurotransmitter receptors. BD 1063 has been shown to antagonize cocaine efffects.
 
SML0637   BD750 ≥98% (HPLC) BD750 is a benzothiazole derivative that inhibits proliferation of T-cells by a mechanism that involves inhibition of STAT5 phosphorylation and expression of cyclin D3 and CDK6. In the presence of BD750, human and mouse T cells stimulated with anti-CD3/CD28, alloantigen, PMA or ConA undergo G0/G1 cell cycle arrest, but express CD25 and CD69 and secrete IL-2 and IL-4. BD750 inhibits delayed-type hypersensitivity in mice.
 
SML0450 5-BDBD ≥98% (HPLC) 5-BDBD is a specific inhibitor of P2X4. The compound inhibits P2X4 currents in CHO cells with an IC50 of 500 nM.
 
B9554   BDS-I ≥95%, lyophilized powder Specifically blocks the rapidly inactivating Kv3.4 channel.
 
SML1384 BEC hydrochloride ≥98% (HPLC) BEC (S-(2-boronoethyl)-l-cysteine) is a potent and specific arginase inhibitor that restores flow-induced responses in arterioles from diabetic rats.
 
B0385 Beclomethasone ≥99% An anti-inflammatory glucocorticoid.
human ... CYP1A2(1544)
V3375 Bee venom from Apis mellifera (honey bee) lyophilized powder    
B0935 Benazepril hydrochloride ≥98% (HPLC), solid Benazepril is a long-acting angiotensin converting enzyme (ACE) inhibitor.
 
B5437 Bendamustine hydrochloride hydrate ≥98% (HPLC) Bendamustine hydrochloride is a DNA-alkylator with a distinct pattern of activity. Bendamustine activates DNA-damage stress response and apoptosis; inhibits mitotic checkpoints; and induces mitotic catastrophe.
 
B6813 Benidipine hydrochloride ≥98% (HPLC) Calcium Channel Blocker
 
B016 Benoxathian hydrochloride solid Selective α1-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
B7283 Benserazide hydrochloride ≥98% (TLC), solid Inhibitor of L-aromatic amino acid decarboxylase.
human ... DDC(1644)
B2417 Benzamil hydrochloride hydrate ≥98% (HPLC) Selective and potent blocker of Na+/H+ and Na+/Ca2+ channels
human ... SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340)
mouse ... Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278)
rat ... Scnn1a(25122), Scnn1b(24767), Scnn1g(24768)
B6936 3-Benzidino-6-(4-chlorophenyl)pyridazine ≥98% (HPLC), solid 3-Benzidino-6-(4-chlorophenyl)pyridazine is an inhibitor of delayed rectifier and transient outward potassium currents. The IC50 values for the blocking action of BCP on IKDR and IKA was calculated as 7.13 μM and 0.55 μM, respectively in acutely isolated rat hippocampal pyramidal neurons by using whole-cell patch-clamp technique. The parent compound, minaprine (Cat. No. M3157), has selective affinity for M1 muscarinic receptors and possesses memory-enhancing properties and also acts as an antidepressant.
 
B2311 5-(2-Benzothiazolyl)-3-ethyl-2-[2-(methylphenylamino)ethenyl]-1-phenyl-1H-benzimidazolium iodide ≥98% (HPLC) 5-(2-Benzothiazolyl)-3-et<WBR>hyl-2-[2-(methylphenylami<WBR>no)-ethenyl]-1-phenyl-1H-<WBR>benzimidazolium, or Akt Inhibitor IV, is a cell-permeable benzimidazole compound that inhibits Akt phosphorylation/activatio<WBR>n by targeting the ATP binding site of a kinase upstream of Akt, but downstream of PI3K. Shown to block Akt-mediated FOXO1a nuclear export (IC<SUB>50</SUB> = 0.625μM) and cell proliferation (IC<SUB>50</SUB> < 1.25μM) in 786-O cells. Unlike phosphatidylinositol analog-based Akt inhibitors, this inhibitor does not affect PI3K.
 
SML1365 4-(Benzothiazol-2-yl)pentenoic acid 13 ≥98% (HPLC) 4-(Benzothiazol-2-yl)pentenoic acid 13 is a cell permeable and potent inhibitor of the Mycobacterium tuberculosis aminotransferase BioA.
 
B8263 Benzphetamine hydrochloride Adrenergic receptor agonist; CNS stimulant.
 
SML0847 Benztropine mesylate ≥98% (HPLC) Benztropine mesylate is a centrally acting muscarinic acetylcholine receptor antagonist and dopamine transporter (DAT) inhibitor (IC50 = 118 nM). Benztropine mesylate has been used to treat the symptoms of Parkinson′s disease and is currently in clincial trials for chronic back pain.
 
UC440 Benzydamine N-oxide hydrogen maleate CYP2C9 substrate
 
SML0532 N-Benzyl-2,4-dinitrobenzenesulfonamide ≥98% (HPLC) N-benzyl-2,4-dinitrobenzenesulfonamide reacts with cysteine to release SO2.
 
B2292 O6-Benzylguanine ≥98% (TLC), solid O(6)-benzylguanine is an antineoplastic agent that binds the DNA repair enzyme O(6)-alkylguanine DNA alkyltransferase (AGT), resulting in inhibition of AGT-mediated DNA repair. It is widely used in various DNA repair mechanism studies and potentiates the effects of other chemotherapeutic agents that damage DNA.
human ... MGMT(4255)
B8686 (+)-N-3-Benzylnirvanol ≥98% (HPLC), powder (+)-N-3-Benzyl-nirvanol is a potent selective CYP2C19 inhibitor. CYP2C19 has a high frequency of drug resistance; highly polymorphic.
 
B2938 BEPP monohydrochloride ≥98% (HPLC) BEPP is a double-strand RNA-dependent protein kinase (PKR) activator. The double-strand RNA (dsRNA)-dependent protein kinase is a ubiquitously expressed serine threonine kinase, inducible by interferon γ. PRK is involved in several curtail cellular regulations including phosphorylation of eIF2α (which leads to inhibition of protein synthesis and eliciting antivirus and antitumor activities), modulating activities of eIF2α, NF-κB, ATF-3, and p53. BEPP also inhibits the growth of a human lung cancer cell line overexpressing PKR.
 
B5016 Bepridil hydrochloride powder Non-selective calcium channel blocker and class IV antiarrhythmic agent; inhibits Na+-Ca2+ exchange; inhibits growth of brain tumor cells in vitro.
 
SML1925 Bepristat 2a hydrochloride ≥95% (HPLC) New Bepristat 2a is a selective reversible inhibitor of protein disulfide isomerase (PDI), an enzyme in the endoplasmic reticulum that catalyzes disulfide bond breakage and reformation to catalyze protein folding. Unlike most PDI inhibitors, Bepristat 2a binds at the substrate-binding site, rather than the catalytic site. Bepristat 2a blocked PDI activity with an IC50 value of 1200 nM, while enhancing catalytic activity of remote PDI domains. PDI is up-regulated in several cancers, has been implicated in neurodegenerative processes, and plays an important role in thrombus formation. Bepristat 2a potently inhibited platelet aggregation and thrombus formation in vivo.
 
SML1737 Beraprost sodium ≥98% (HPLC) Beraprost sodium is a chemically stable analog of prostacyclin PGI2. As other prostanoids, beraprost is a potent vasodilator and possesses antithrombotic, antiproliferative and anti-inflammatory properties. Beraprost sodium activates prostaglandin I (IP) receptor, which is coupled with Gs proteins and activates adenylate cyclase. It has been studied for the treatment of pulmonary hypertension.
 
SML1608 Besifloxacin hydrochloride ≥98% (HPLC) Besifloxacin is a broad spectrum fourth-generation fluoroquinolone antibiotic. Besifloxacin is effective against gram positive and negative, aerobic and anerobic bacteria. Fluoroquinolones stabilize DNA strand breaks created by DNA gyrase and topoisomerase IV by binding to the enzyme-DNA complex generating persistent, covalent enzyme–DNA adducts, inhibiting DNA synthesis. Besifloxacin inhibits both DNA gyrase and topoisomerase IV at nearly equal concentrations. It is used clinically primarily in the treatment of bacterial conjunctivitis.
 
SML0163   Beta-3 Adrenoceptor Partial Agonist (β3-633-AG) synthetic This ligand is a partial agonist at β3 adrenoceptors, is a very weak partial agonist at β1, and has no agonist activity at β2. It also acts as an antagonist at β1, β2 and β3.
 
B7005 Betamethasone ≥98%   human ... ABCB1(5243), CYP3A4(1576), IL4(3565), IL5(3567), NR3C1(2908)
mouse ... Abcb1a(18671), Abcb1b(18669), Ifng(15978), Nos2(18126), Tnf(21926)
rat ... Ar(24208), Nr3c1(24413), Tnf(24835)
B1152   Betamethasone 17,21-dipropionate Betamethasone 17,21-dipropionate is a glucocorticoid with anti-inflammatory and immunosuppressive activity.
 
B7652 Betamethasone 21-phosphate disodium ≥97%    
B0515 Betamethasone 17-valerate Betamethasone 17-valerate is a glucocorticoid with anti-inflammatory and immunosuppressive activity.
 
B5683 Betaxolol hydrochloride >98% (HPLC) Selective β1 adrenoceptor antagonist.
human ... ADRB1(153)
SML0558 BETP ≥98% (HPLC) BETP is a positive allosteric modulator of the GLP-1 receptor that potentiates cAMP accumulation and glucose-dependent insulin release in pancreatic islet cells, in the presence of the weak GLP-1 metabolite, GLP-1(9-36). BETP has additive effects on the endogenous GLP-1 receptor ligand GLP-1(7-36).
 
SML0282 Bexarotene ≥98% (HPLC) Bexarotene is a highly selective retinoid X receptor (RXR) agonist. It is an antineoplastic agent, already approved as an oral antineoplastic agent for cutaneous T cell lymphoma and being investigated against other cancers. A study has found that bexarotene in a mouse Alzheimer′s model lowered the most toxic form of β-amyloid peptide and increased cognitive ability. The activity in the mouse Alzheimer′s models are believed to be by activating PPARγ:RXR and LXR:RXR dimers which induces the expression of apoE and facilitates Aβ clearance and promotes microglial phagocytosis.
 
B7273 Bezafibrate ≥98%, solid The peroxisome proliferator-activated receptor (PPAR) is a member of the steroid nuclear receptor superfamily. Bezafibrate is a peroxisome proliferator-activated receptor agonist for PPARα, PPARδ, and PPARγ. Lipoprotein lipase (LPL) activator.
PPARgamma agonists, including Bezafibrate, have beneficial effects in the suppression of the inflammatory response during RSV infection and therefore might have clinical efficacy in the course of severe RSV-infection.
human ... HBA2(3040), PPARA(5465), PPARD(5467), PPARG(5468)
mouse ... Ppara(19013), Ppard(19015), Pparg(19016)
B4311 BF-170 hydrochloride ≥98% (HPLC), solid BF-170 is a new probe for neurofibrillary tangles (tau fibrils). It exhibits greater binding affinity to tau than to Aβ fibrils, EC50 = 221 nM vs. EC50 = 786 nM (Ki for Aβ > 5,000 nM). BF-170 demonstrates fast clearance from the brain; clearly visualizes neurofibrillary tangles, neuropil threads, and paired helical filament-type neuritis. BF-70 may become one of the candidate compounds for in vivo imaging of tau pathology associated with Alzheimer′s disease and is a useful tool in distinguishing among tau and Aβ fibrils specifically in AD.
 
SML1703 2-BFI hydrochloride ≥98% (HPLC) 2-BFI is a high-affinity Imidzoline I2 receptor ligand (Ki = 9.8 nM) In an in vivo functional assay, 2-BFI induces hypothermia in rats.
 
SML0867   BG45 ≥98% (HPLC) BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM) over HDAC1, 2. BG45 did not inihibit HDAC6. BG45 signigicantly inhibited tumor growth in a mouse model of multiple myeloma either alone and synergistically in combination with bortezomib.
 
B4813 BGP-15 ≥98% (HPLC) BGP-15 is PARP inhibitor, HSP72 activator.
 
B8809 BH3I-1 ≥97% (HPLC), powder, yellow BH3I-1is a synthetic cell permeable Bcl-xL antagonist; apoptosis inducer.
 
SML0275 rac BHFF ≥98% (HPLC) rac BHFF is an orally active, potent and selective positive allosteric modulator of GABA-B. rac BHFF increases the potency and efficacy of GABA.
 
B162 B-HT 920 dihydrochloride solid, ≥98% (HPLC) α2-adrenoceptor agonist; D2 dopamine receptor agonist.
rat ... Drd2(24318)
B0186 BI-6C9 ≥97% (HPLC), solid BI-6C9 is a tBid inhibitor and antiapoptotic.
 
B3063 BI-78D3 ≥98% (HPLC) BI-78D3 is a substrate competitive inhibitor of JNK. JNK′s binds to JNK-interacting protein-1 (JIP1) (scaffolding protein) through high affinity D-domain on JIP1. This interaction is needed to place JNK next to target protein. BI-78D3 is a mimetic of a critical peptide structure of JIP1 which binds to JNK away from ATP binding domain preventing JIP1 JNK interaction thus acting as a substrate competitive inhibitor both in vitro and in vivo. The compound represents a growing number of modern kinase inhibitors acting at protein protein interacting areas (scaffolding) rather than ATP binding pockets.
 
SML0489 BI-87G3 ≥98% (HPLC) BI-87G3 is a cell-permeable, potent and selective competitive inhibitor of the c-Jun N-terminal kinase (JNK). BI-87G3 is a JNK inhibitor that targets the JIP-JNK interaction site.
 
SML1655 BI-9564 ≥97% (HPLC) BI-9564 is a cell permeable, potent and specific inhibitor of BRD9 and BRD7. For full characterization details, please visit the BI-9564 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
B5435 BIA 2-093 ≥98% (HPLC), solid Blocker of voltage-gated sodium channels; significantly blocks excitatory amino acid (glutamate and aspartate) release.
rat ... Scnn1g(24768)
SML0306 Biapenem ≥98% (HPLC) Biapenem is a broad spectrum, carbapenem-based antibiotic with activity against both Gram-positive and Gram-negative bacterial strains.
 
B174 BIBP 3226 Selective non-peptide neuropeptide Y1 (NPY1) receptor antagonist.
 
B9061 Bicalutamide (CDX) ≥98% (HPLC), powder Bicalutamide (CDX) is a non-steriodal Androgen Receptor (AR) antagonist and a pure antiandrogen. It acts via balancing histone acetylation/deacetylation and recruitment of coregulators. Bicalutamide (CDX) abolishes androgen-mediated expression. For example, MMP13 upregulation in prostate cancer, PLZF (promyelocytic leukemia zinc finger protein), and GADD45γ (growth arrest and DNA damage inducible, gamma). Bicalutamide (CDX) is inhibited by non-genomic, transcription-independent stimulation of PI3K/AKT phosphorylation by androgens.
 
B8435 BiCAPPA ≥97% (HPLC), solid Inhibitor of the formation of abnormal ß-rich isoform of prion protein PrPSc.
 
14340 (+)-Bicuculline ≥97.0% (TLC) (+)-Bicuculline is a GABAA receptor antagonist.
(+)-Bicuculline is a GABAA receptor antagonist, which acts as a competitive inhibitor of GABA liganding binding to the receptor.
rat ... Gabra2(29706)
B7561 1(S),9(R)-(−)-Bicuculline methbromide ≥98% (HPLC), solid 1(S),9(R)-(−)-Bicuculline methbromide is a GABAA receptor antagonist, which blocks Ca2+-activated potassium (SK) channels. It is the water-soluble derivative of (+)-bicuculline.
 
B7686 1(S),9(R)-(−)-Bicuculline methchloride ≥97% (HPLC), powder 1(S),9(R)-(−)-Bicuculline methchloride is a GABAA receptor antagonist, which blocks Ca2+-activated potassium (SK) channels.
 
14343 1(S),9(R)-(−)-Bicuculline methiodide ≥95.0% (HPCE) (-)-Bicuculline methiodide is a GABAA receptor antagonist, which acts as a competitive inhibitor of GABA ligand binding to the receptor.
 
B3313 Bicyclol ≥98% (HPLC) Bicyclol is a anti-hepatitis drug, used in China for chronic hepatitis B and presumably C. The drug appears to protect against liver injury in animals. Recently it was reported that bicyclol induce the expression of hepatic HSP27 and HSP70, and thus consequently inhibits the transcription factor NF-?B-mediated apoptosis and necrosis in liver tissue. It appears that bicyclol induces hepatic HSP27 and HSP70 expression through activating transcription of HSPs genes.
 
SML1670 Bifeprunox mesylate ≥98% (HPLC) Bifeprunox (DU-127,090) is an atypical antipsychotic. Bifeprunox is a dopamine D2 receptor (D2R) partial agonist that exhibits 5-HT1A agonist properties.
 
B3563 Bifonazole ≥98% (HPLC) Bifonazole is an imidazole-based anti-fungal agent with broad spectrum activity against many fungi, molds, yeast and some Gram-positive bacteria. Bifonazole inhibits ergosterol biosynthetic protein 28 and Cytochrome P450 2B4.
 
SML1411 BIHC ≥98% (HPLC) BIHC is a potent TNF blocker that inhibits the proliferation of various HCC cells. BIHC exhibits potent cytotoxic activity against the HepG2 cell line while showing less toxicity towards normal hepatocytes.
 
SML0724   Bikaverin from Fusarium subglutinans, ≥98% (HPLC) Bikaverin is a red pigment with a polyketide tetracyclic benzoxanthone structure. Bikaverin has an antibiotic activity against some protozoa and fungi and also inhibits Succinate- and NAD-linked respiration in rat mitochondria at 20 mg/mL. At higher concentrations (50 mg/mL) it acts as an oxidative phosphorylation uncoupling agent of tumor cells and isolated rat liver mitochondria. Bikaverin demonstrates antitumor activity on Erlich ascites carcinoma (EAC), leukemia and sarcoma cells.
 
SML0094 Bikinin ≥98% (HPLC) Bikinin is a strong activator of brassinosteroid (BR) signaling. It is an Arabidopsis GSK-3 Inhibitor, an Arabidopsis SHAGGY-related Kinase Inhibitor, and a GSK-3-like Kinase BIN2 Inhibitor. Bikinin directly inhibits BIN2 (group II GSK3s) by interfering with ATP binding. Bikinin is specific toward a subset of Arabidopsis GSK3 kinases including BIN2 and ASK α, γ, ε, ι, and θ.
 
SML0528 BIM5078 ≥98% (HPLC) BIM5078 is a potent Hepatocyte nuclear factor 4a (HNF4a) antagonist that directly binds to ligand-binding pocket and modulates the expression of known HNF4a target genes. BIM5078 also inhibits insulin gene expression by disruption of E47 and PDX-1 binding to insulin promoter. BIM5078 is selectively cytotoxic to transformed cells.
 
B4063 BIMU8 hydrate ≥98% (HPLC) BIMU8 hydrate is a potent 5-HT4 serotonin receptor agonist. Serotonin (5-HT) is a major neurotransmitter that acts through a family of GPCRs and one ion channel. 5-HT4 receptor is GPCR expressed in many tissues, including brain, and modulates dopamine secretion, learning, and memory. BIMU8 is a full agonist at 5-HT4, but it binds differently than the endogenous ligand, 5-HT, shown through site-directed mutagenesis studies. It depolarizes neurons and was used to localize 5-HT4 to somatic but not dendritic regions of CA1 pyramidal neurons.
 
N1771 nor-Binaltorphimine dihydrochloride Potent and highly selective κ opioid receptor antagonist.
human ... OPRK1(4986)
B1186 Binucleine 2 ≥97% (HPLC) Binucleine 2 is a cytokinesis inhibitor.
 
B1686 BIO ≥98% (HPLC) 6-bromoindirubin-3′-oxime (BIO) is a potent, reversible and ATP-competitive GSK-3α/β inhibitor and the first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells. Human embryonic stem cells (hESCs) are maintained in the undifferentiated state through treatment with a GSK-3 inhibitor, BIO, under a feeder-free condition.
 
SML0531 BIO-Acetoxime ≥98% (HPLC) BIO-Acetoxime is a potent and selective GSK-3a/b inhibitor that reduces invasiveness of gliomas and extends animal survival in intracranial glioma models. Also, BIO-Acetoxime induces Wnt signaling and inhibits CD8+ T cell effector differentiation.
 
SML1031   Bioymifi ≥98% (HPLC) Bioymifi induces apoptosis via the Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) death receptor DR5 independent of TRAIL. Bioymifi binds selectively to the extracellular domain of DR5 with little binding affinity to DR4, promoting DR5 aggregation and activation. Bioymifi caused apoptosis and cell death in a variety of human cancer cell lines including T98G human glioblastoma cells, lung cancer cell lines H460 and H1155, the cervical cancer cell line HeLa, the osteosarcoma cell line U2OS, the pancreatic carcinoma cell line Miapaca and the colon cancer cell line HT29.
 
SML0265 BIP-135 ≥95% (HPLC) BIP-135 is a potent inhibitor of glycogen synthase kinase-3 (GSK3) found to be relatively selective for GSK-3β (21 nM) over GSK-3α with modest activity toward PKCβ (β1: 980 nM; β2: 219 nM), DYRK1B (590 nM), and PI3Kα (870 nM). BIP-135 was found to be a superior neuroprotective agent in a cortical neuron model of oxidative stress over other GSK-3 inhibitors, such as AR-A011418 and SB216763. In a mouse model of spinal muscular atrophy (SMA), BIP-135 elevated SMN protein levels in vitro and extended median survival.
 
B5311 Biperiden hydrochloride ≥98% (HPLC), powder Biperiden hydrochloride is antiparkinsonian; non-selective muscarinic receptor antagonist. It is used for the adjunctive treatment of all forms of Parkinson′s Disease (postencephalitic, idiopathic, and arteriosclerotic); also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy. LD50 in rats 750 mg/kg; in dogs 340 mg/kg.
 
SML0299 Biphalin trifluoroacetate salt ≥97% (HPLC) Biphalin is a dimeric enkephalin that is a potent and non-selective opioid receptors (OR) agonist. It displays a high analgesic potency that is over 1000-fold greater than morphine. Studies show that biphalin exhibits neuroprotective effects in rat models of stroke.
 
B8688 Biphenyl-indanone A ≥98% (HPLC), powder Biphenyl-indanone A (BINA) is a potent selective positive allosteric modulator for the group II metabotropic glutamate receptor subtype mGluR2. In animal studies BINA showed anxiolytic and antipsychotic effects, and blocked the effects produced by the hallucinogenic drug DOB. It decreased cocaine self-administration in rats, with no effect on food self-administration. In recombinant systems, BINA selectively potentiated the response of mGluR2 to glutamate with no effect on the glutamate response of other mGluR receptor subtypes tested.
 
SML1811 BIQ ≥98% (HPLC) BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD). BIQ induces significant and reversible plasma erythropoietin (EPO) levels in vitro and in hemodialysis patients.
 
A9013 1,5-Bis(4-allyldimethylammoniumphenyl)pentan-3-one dibromide Selective acetylcholinesterase inhibitor.
human ... ACHE(43)
A5581 3,3-Bis(aminoethyl)-1-hydroxy-2-oxo-1-triazene ≥95%    
B4563 Bisantrene dihydrochloride ≥98% (HPLC) Bisantrene dihydrochloride is an antineoplastic agent, MDR1 substrate, DNA intercalator, and topoisomerase II poison. Cancer cells that develop resistance to bisantrene tend to overexpress P-glycoprotein. Bisantrene can be used to select for P-glycoprotein-mediated multiple drug resistance. The data suggest that bisantrene is an excellent substrate for P-glycoprotein.
 
B1155 bisBenzimide H 33258 powder, BioReagent, suitable for cell culture, ≥98% (HPLC and TLC) bisBenzimide H 33258 is a potent and selective Bcl-XL inhibitor. bisBenzimide H 33258 is a membrane-permeable, fluorescent DNA stain with low cytotoxicity that intercalate in A-T regions of DNA.
 
SML0404 6,8-Bis(benzylthio)-octanoic acid ≥98% (HPLC) CPI-613 is an E1α pyruvate dehydrogenase (PDH) modulator that prevents cancer cells from metabolizing glucose for energy. CPI-613 has been granted orphan drug status by the US FDA for pancreatic cancer.
 
B6938 Bisdemethoxycurcumin ≥98% (HPLC), solid Bisdemethoxycurcumin (BDMC) is a derivative or curcumin, and represents one of the major active components of curcumin products isolated from Curcumae sp. BDMC shares similar anti-inflammatory properties with demethoxycurcumin. It inhibits LPS-induced nitric oxide (NO) production and expression of iNOS and COX2 in RAW264.7 cells by blocking NF-kB activation. BDMC also displays unique properties in that it enhances Abeta clearance by upregulating expression MGAT3 and TLR genes. BDMC potently inhibits AKR1B10.
 
SML0819   Bisdionin C ≥98% (HPLC) Bisdionin C is a cell-permeable, competitive acidic mammalian chitinase (AMCase) and chitotriosidase (CHIT1) inhibitor. Bisdionin C also potently inhibits bacterial AfChiB1 chitinase.
 
SML1598 Bis(heptyl)-cognitin dihydrochloride ≥98% (HPLC) Bis(heptyl)-cognitin (B7C) is a potent neuroprotective agent and cognitive enhancer. It is thought to have multiple mechanisms of action including inhibition of AChE, and inihbititon of the amyloid precursor protein/beta-amyloid cascade. It has been shown to inhibit the formation of Aβ1-42 oligomers and reduce the amount of pre-formed Aβ1-42 oligomers, and to induce robust neurite outgrowth in PC12 cells.
 
H5915 2,3-Bis(4-hydroxyphenyl)propionitrile ≥98% (HPLC) 2,3-Bis(4-hydroxyphenyl)-propionitrile (Diarylprepionitrile, DPN) is an ERβ-selective agonist; IC50 = 15nM. DPN protects WT and ARKO mice and significantly decreases IL-1β following LPS treatment in young adult-derived microglia. PPT (Cat. No.H6036, ERa agonist) enhances cell proliferation, while DPN inhibits it. PPT increases Bcl-2 expression, while DPN decreases it. DPN also elevates Bax expression. DPN induces a dose-dependent increase on vitellogenin synthesis. PPT and DPN are effective in dynamically, but differentially regulating intracellular calcium signaling in hippocampal neurons. DPN is more efficacious than PPT in potentiating a physiological concentration of glutamate-induced intracellular Ca2+ rise in these neurons. DPN prevents the development of prostatic hyperplasia and inflammation in testosterone-treated LuRKO mice.
 
B3056 Bisindolylmaleimide II ≥97% (Mixture of 2 isomers) Inhibitor of protein kinase C.
 
B3306   Bisindolylmaleimide IV ≥98% (TLC), solid Inhibitor of protein kinase C.
human ... CDK2(1017), EGFR(1956)
rat ... Prkca(24680)
B3681 Bisindolylmaleimide VII 96% (TLC), solid Selective inhibitor of protein kinase C.
 
B3931 Bisindolylmaleimide X hydrochloride ≥90%, solid Selective inhibitor of protein kinase C.
 
B4056 Bisindolylmaleimide XI hydrochloride ≥98% (TLC), solid Selective inhibitor of protein kinase C.
 
SML0959   Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene ≥98% (HPLC) Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene is a non-covalent inhibitor of the interaction between Kelch-like ECH-associated protein 1 (Keap1) and nuclear factor erythroid 2-related factor 2 (Nrf2). The Keap1–Nrf2 protein–protein interaction is considered a critical point of the Keap1–Nrf2–ARE (antioxidant response elements) system that protects cells from oxidative stress. Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene prevents Keap1 repression of Nrf2 activation, allowing Nrf2 to initiate antioxidant response element (ARE) to protect the cell. Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene has an IC50 of 2.7 micromolar and specifically binds to the Keap1 Kelch-DC domain.
 
B2185 Bisoprolol hemifumarate salt ≥98% (HPLC), solid Cardioselective β1-adrenoceptor antagonist.
 
D3415 Bisphenol A diglycidyl ether PPARγ inhibitor that blocks rosiglitazone- and insulin-induced adipogenesis.
 
SML1440 Bithionol ≥98% (HPLC) Bithionol was originally used as an anthelmintic. Bithionol has more recently been investigated for potential use as an anti-ovarian cancer drug and as a possible treatment for Alzheimer′s disease. Bithionol inhibited Aβ42 seeding capacity and fibril growth, stabilized diffuse amyloid plaques, reduced the levels of Aβ42 oligomers and ameliorated synapse loss, neuronal damage and astrogliosis in a transgenic mouse model of Alzheimer′s disease. Bithionol appears to act through several mechanisms of action including uncoupling of oxidative phosphorylation, ROS generation, NF-κB inhibition, autotaxin inhibition, and as an activator of Slack sodium-activated potassium (KNa) channels.
 
SML1051   Bivalirudin trifluoroacetate salt ≥97% (HPLC) Bivalirudin is a specific and reversible bivalent direct thrombin inhibitor. Bivalirudin specifically binds to both the catalytic site and to the anion-binding exosite of circulating and clot-bound thrombin.
 
SML1073 BIX ≥98% (HPLC) BIX (BiP protein inducer X) induces the expression of the endoplasmic reticulum chaperone protein GRP78 (glucose regulated protein 78, BiP) leading to an attenuation of the unfolded protein response. BIX protects neuronal cells and retinal cells from ER-stress induced cell death.
 
B9311 BIX 01294 trihydrochloride hydrate ≥98% (HPLC), powder BIX 01294 is a selective histone methyl transferase inhibitor. In its inhibition of the histone lysine methyltransferases, BIX 01294 does not compete with cofactor S-adenosyl-methionine. The target enzyme is G9a, and it selectively impairs G9a HMTase and the generation of H3K9me2 in vitro.
 
B5313 BIX-01338 hydrate ≥98% (HPLC) BIX-01338 is a non-selective histone lysine methyltransferase inhibitor.
 
B2186 BL-1249 ≥98% (HPLC) BL-1249 is a putative activator of potassium TREK-1 channel.
 
B0560 (−)-Blebbistatin solid, synthetic (-)-Blebbistatin is a cell cycle inhibitor; selective inhibitor of non-muscle myosin II.
 
B5507 Bleomycin sulfate from Streptomyces verticillus crystalline, 1.5-2.0 units/mg solid Bleomycin sulfate binds to DNA, causes ssDNA scission at specific base sequences and inhibits DNA synthesis. This inhibitory action requires bleomycin to bind oxygen and a metal ion. It can also cleave RNA, to a lesser degree but more selectively. It acts as an inducer and regulator of apoptosis and inhibits tumor angiogenesis.
 
PZ0022 BLI-489 hydrate ≥98% (HPLC) BLI-489 is a penem β-lactamase inhibitor, which has shown activity against class A, C, and D β-lactamases. BLI-489 is being tested in combination therapy for drug-resistant bacteria.
 
B7188 Blonanserin ≥98% (HPLC) Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
 
SML0059 BLT-1 ≥98% (HPLC) Block lipid transport-1 (BLT-1) is a specific inhibitor of the SR-BI (Scavenger receptor, class B, type I) mediated lipid transfer. The compound inhibits both cellular selective lipid uptake of HDL cholesteryl ether and efflux of cellular cholesterol to HDL.
 
SML0512 BLT-4 ≥98% (HPLC) BLT-4 is a blocker of lipid transport-4 (BLT-1). BLT-4 is a specific, reversible inhibitor of SR-BI (Scavenger receptor, class B, type I) mediated lipid transfer. The molecule blocks the cellular uptake and transfer of cholesterol ester from HDL.
 
B8685 BM 15766 sulfate ≥98% (HPLC), powder Dehydrocholesterol reductase inhibitor. Inhibits 7-dehydrocholesterol reductase, which catalyzes the last step of cholesterol synthesis.
 
SML1183 BMH-21 ≥98% (HPLC) BMH-21 is a potent inhibitor of RNA Pol I. BMH-21 binds strongly to GC-rich DNA sequences, ultimately inhibiting RNA Pol I, blocking transcription and disrupting the nucleolar structure. BMH-1 causes dissociation of the RPA194 catalytic subunit from Pol I, and disassembly of Pol I:DNA complexes. The compound BMH-21 inhibits proliferation of a broad range of tumor cell lines.
 
B8063 BML-210 ≥98% (HPLC), powder BML-210 is a histone deacetylase inhibitor. Treatment of A549 cells with BML-210 results in a dose-dependent increase in acetylated histone levels (EC50 = 36 μM). In HeLa extracts, the IC50 for inhibition of HDAC activity is 80 μM.
 
SML1079   BMOV ≥95% (elemental analysis) BMOV is a potent, orally available vanadium complex that acts as insulin mimetic. Apparently, BMOV anti-diabetic effect results from enhancement of the tyrosine-phosphorylation of insulin receptor by inhibition of the protein tyrosine phosphatase-1B (PTP-1B). In diabetic rats BMOV restores normoglycaemia without rising insulin levels. BMOV is a potent phosphatase inhibitor.
 
SML1582   BMS-3 ≥95% (HPLC) BMS-3 shows cytotoxic effects not related to LIMK, but rather through reduction of the levels of tubulin transcripts and induction of mitotic arrest.
It is a specific inhibitor of LIMK1. LIMK1 is responsible for the inactivation of cofilin (ADF family protein), leading to actin reorganization. It is upregulated in several invasive cancers.
 
SML0708   BMS-182874 hydrochloride ≥98% (HPLC) BMS-182874 is a potent selective nonpeptide endothelin ETA receptor antagonist. BMS-182874 is 1000-fold selective for ETA over ETA B receptors with a Ki of 48 nM for ETA receptors vs >50 μM for ETB.
 
SML1149 BMS-189453 ≥98% (HPLC) BMS-189453 is a potent RARβ agonist that acts as an antagonist against RARα and RARγ. BMS-189453 induces RARβ reporter gene expression at sub nanomolar levels, and is 30 fold more potent than all-trans retinoic acid for inducing TGFβ activity in normal breast cells. The compound BMS-189453 does not transactivate RARα or γ transcriptional activity, but binding to those family members induces a strong transrepression of phorbol ester-induced AP-1 activity (IC50 = 0.1 nM in HeLa and MCSF-7). BMS-189453 significantly increases the efficiency of cardiac differentiation of hESCs.
 
SML0866   BMS-191011 ≥98% (HPLC) BMS-191011 is a potent opener of BKCa opener (large-conductance Ca2+-activated K channel). The compound BMS-191011 has neuroprotective properties in rodent models of stroke, and induces dialation of rat retinal arterioles.
 
BM0012 BMS-191095 hydrochloride ≥98% (HPLC) BMS-191095 is a potent and selective mitochondrial ATP-sensitive K1 channel (KATP) channel opener devoid of peripheral vasodilating activity. BMS-191095 improves postischemic recovery of function and reduced lactate dehydrogenase release in the isolated rat hearts.
 
B5063 BMS-193885 ≥98% (HPLC) BMS-193885 is a potent, selective Y1 antagonist that is active in both acute and chronic animal models of food intake. Although it is active in vivo, it is not orally bioavailable due to poor intestinal absorption, so it is not being pursued for pharmaceutical development. BMS-193885 has been used as a pre-clinical proof of concept tool for showing efficacy of Y1 antagonism in treating obesity.
 
SML1084 BMS-195614 ≥97% (HPLC) BMS-195614 (BMS614) is a potent neutral retinoic acid receptor RARα selective antagonist with an IC50 of 2.5 nM.
 
BM0017 BMS-199264 hydrochloride ≥98% (HPLC) BMS-199624 is a potent inhibitor of the ATP hydrolase activity of mitochondrial F1F0 ATP synthase. The compound BMS-199624 has no affect on the ATP synthase function of F1F0. In isolated rat hearts, BMS-199624 blocks depletion of ATP levels, and blocks necrosis during ischemia.
 
SML1313 BMS 204352 ≥98% (HPLC) BMS 204352 is a potassium channel modulator. Originally developed as a potent opener of large-conductance, calcium-activated (Maxi-K, KCa1.1, BK) potassium channels, BMS 204352 also acts as a positive modulator at Kv7 (KCNQ) channels.
 
BM0014 BMS-207940 ≥98% (HPLC) BMS-207940 is a very potent and selective ETA endothelin receptor antagonist. BMS-207940 has a Ki of 10 pM for ETA, 80000-fold selective for ETA vs ETB.
 
BM0008 BMS-214662 hydrochloride ≥98% (HPLC) BMS-214662 is an orally available, potent and selective inhibitor of farnesyltransferase that reduces Ras prenylation in NF90-8 and ST88-14 sheath tumor (MPNST) cell lines. BMS-214662 induces apoptosis in cancer cell lines, and potently inhibits growth of human tumor xenografts.
 
BM0030   BMS-248360 ≥98% (HPLC) BMS-248360 is an orally active dual antagonist of angiotensin II subtype 1 (AT1) and endothelin subtype A (ETA) receptors. BMS-248360 exhibited a broader spectrum of antihypertensive activity when compared to individual AT1 or ETA receptor antagonists.
 
BM0013 BMS-281384 bis-HCl ≥98% (HPLC) BMS-281384 is a selective and potent phosphodiesterase 5 (PDE 5) inhibitor. BMS-281384 was found to have an IC50 value of 0.8 nM for PDE5 and 47 to 9200-fold selective over other PDEs 1-6.
 
SML0210   BMS-299897 ≥98% (HPLC) BMS-299897 is a potent inhibitor of γ-secretase. The comound is 15-fold more selective for inhibiting the cleavage of b-amyloid precursor protein over Notch cleavage (IC50s 7.1 and 105.9, respectively). In vivo,BMS-299897 blocks the formation of Aβ40 and Aβ42 in the brain and CSF without affecting maturation of CD8+ T cells or intestinal goblet cells, suggesting Notch signalling was not significantly inhibited.
 
SML0784   BMS-303141 ≥98% (HPLC) BMS-303141 is a potent inhibitor of ATP citrate lyase (ACL). BMS-303141 inhibits lipid synthesis in HepG2 cells with an IC50 of 8 μM, and lowers plasma triglycerides in a murine hyperlipdemia model.
 
BM0015 BMS-309403 ≥98% (HPLC) BMS-309403 is a potent and selective inhibitor of fatty acid binding protein 4 (FABP4), also known as adipocyte FABP (A-FABP, aP2). FABP4 is an intracellular lipid-binding protein responsible for the transportation of fatty acids. It is expressed primarily in adipose tissue and is associated with inflammation, obesity, diabetes and cardiovascular diseases. BMS309403 interacts with the fatty-acid-binding pocket within the interior of FABP4 and has been shown to competitively inhibit fatty acid binding with a Ki value < 2 nM. BMS309403 is orally active and has been shown to reduce atherosclerosis in mice studies.
 
BM0001 BMS-341400 methanesulfonate ≥98% (HPLC) BMS-341400 is a selective and potent phosphodiesterase 5 (PDE 5) inhibitor. BMS-341400 has an IC50 value of 0.3 nM and is 150-fold selective for PDE5 over PDE6 and over 10,000-fold selective for PDE5 over PDE1, PDE2, PDE3, and PDE4.
 
B9935 BMS-345541 ≥98% (HPLC), powder BMS-345541 is an IKB kinase (IKK) allosteric site inhibitor.
 
BM0022 BMS-433771 bis-hydrochloride monohydrate ≥98% (HPLC) BMS-433771 bis-hydrochloride monohydrate is a respiratory syncytial virus (RSV) fusion inhibitor with an EC50 value of 10-12 nM. BMS-433771 bis-hydrochloride targets the RSV fusion (RSVF) protein, preventing viral entry. BMS-433771 bis-hydrochloride is orally available.
 
B6688 BMS 493 ≥98% (HPLC) BMS 493 is an inverse pan-RAR agonist. Retinoic acid receptors (RARs) are ligand-dependent transcription factors that control a number of physiological processes. RARs exert their functions by regulating gene networks controlling cell growth, differentiation, survival, and death.
 
BM0028 BMS-536924 ≥98% (HPLC) BMS-536924 is a potent, orally active, ATP-competitive insulin-like growth gactor-1 receptor (IGF1R) inhibitor that shows anticancer activities in preclinical models.
 
BM0025   BMS-538305 L-(+)-tartrate ≥98% (HPLC) BMS-538305, a saxagliptin analog, is a potent and selective dipeptidyl peptidase IV (DPP-IV) inhibitor.
 
SML1494 BMS-599626 ≥98% (HPLC) BMS-599626 is a potent inhbitor of human epidermal growth factor receptors 1 and 2 (HER1 and HER2, IC50 = 20 and 30 nM, respectively). BMS599626 inhibits proliferation of several HER-expressing cancer cell lines, including HER2-overexpressing breast cancer lines, but does not affect the proliferation rate of HER-negative cancer cell lines.
 
BM0020 BMS-646786 ≥98% (HPLC) BMS-646786 is a potent and specific inhibitor of P2Y1 purinergic receptor that inhibits ADP-mediated platelet aggregation in human blood samples. BMS-646786 significantly reduces thrombus weight in a rat arterial thrombosis model with a limited effect on bleeding.
 
BM0033   BMS-665053 ≥98% (HPLC) BMS-665053 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 </= 1.0 nM against 150 pM ovine CRF for binding human and rat CRF-R1), potency (IC50 = 4.9 nM against 1 nM CRF-stimulated cAMP production in human Y-79 retinoblastoma cells), and selectivity, displaying no affinity toward CRF-R2/CRF2 (IC50 >10 μM against 150 pM ovine CRF in binding assay). BMS-665053 exhibits anxiolytic efficacy in a defensive withdrawal anxiety test in rats in vivo (10 mg/kg p.o.) with good oral bioavailability (F = 52%).
 
SML0286 BMS 753 ≥98% (HPLC) BMS 753 is a very potent, specific agonist for RARa (Ki = 2 nM). BMS 753 does not display significant effects on RARg in reporter based assays, or in binding assays measuring displacement of labeled retinoic acid.
 
BM0003 BMS-754807 ≥98% (HPLC) BMS-754807 is an orally available and potent dual insulin-like growth factor factor-1 receptor (IGF-1R)/ insulin receptor (InsR) tyrosine kinase inhibitor that synergistically enhances antiproliferative effects of 4-hydroxytamoxifen, letrozole, and fulvestrant in MCF-7/AC-1 cells.
 
BM0031   BMS-763534 ≥98% (HPLC) BMS-763534 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 = 0.26 &amp; 0.4 nM against 150 pM ovine CRF for binding rat &amp; human CRF-R1, respectively), potency (IC50 = 1.0 nM against 0.3 nM CRF-stimulated ATCH secretion from primary rat anterior pituitary cells), and selectivity, displaying little affinity toward porcine CRF-R2/CRF2 and 46 other receptor/channel/transporter proteins (IC50 >10 μM). BMS-763534 inhibits CRF-stimulated cAMP production in human Y-79 retinoblastoma cells in cultures (pA2 = 9.47) and exhibits anxiolytic efficacy in a rat situational anxiety model in vivo (0.5-3 mg/kg p.o.).
 
BM0034   BMS-764459 ≥98% (HPLC) BMS-764459 is a pyrazinone-containing antagonist that targets corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) with high affinity (IC50 = 0.86 nM against 150 pM ovine CRF for binding rat CRF-R1), potency (IC50 = 1.9 nM against 1 nM CRF-stimulated cAMP production in human Y-79 retinoblastoma cells), and selectivity, displaying little affinity toward CRF-R2/CRF2 and 43 other receptor/channel/transporter proteins (IC50 >10 μM). BMS-764459 exhibits anxiolytic efficacy in a rat defensive withdrawal model of anxiety in vivo (1-3 mg/kg p.o.) with good oral bioavailability (F in dogs = 53% with 2 mg/kg in suspension and 70% with 3 mg/kg in solution).
 
BM0023 BMS-770767 ≥98% (HPLC) BMS-770767 is an inhibitor of 11-betahydroxysteroid dehydrogenase type I (11β-HSD1), which is a regulator of glucocorticoid activity and thought to play a possible role in metabolic syndrome. 11β-HSD1 can convert cortisol to the inactive metabolite cortisone, or catalyze the reverse reaction, converting inactive cortisone into active cortisol in cells. BMS-770767 was in clinical trials for hypercholesterolemia and Type 2 diabetes.
 
BM0019 BMS-777607 ≥98% (HPLC) BMS-777607 is an ATP-competitive inhibitor of the Met kinase superfamily with IC50 values of 1.8, 3.9, 4.3, and 1.1 nM, respectively, for Ron, Met, Tyro-3, and AxI kinases. BMS-777607 has been studied in a variety of cancer models and has shown anti-cancer activity, causing increased apoptosis, and decreased proliferation and migration, although it has also been shown to induce polyploidy, which may lead to chemoresistance.
 
BM0024   BMS-823778 ≥98% (HPLC) BMS-823778 is an orally available potent and selective inhibitor of 11-β-hydroxysteroid-dehydrogenase 1 (11βHSD-1). BMS-823778 is an antihyperglycaemic.
 
BM0027   BMS-870145 ≥98% (HPLC) BMS-870145 is an orally available, potent and selective P2Y1 purinergic receptor antagonist. BMS-870145 demonstrated similar antithrombotic efficacy with less bleeding compared with P2Y12 antagonist prasugrel in rabbits.
 
BM0018 BMS-906024 ≥98% (HPLC) BMS-906024 is a γ-secretase inhibitor and pan-Notch inhibitor with antineoplastic activity. BMS-906024 is being studied as an anticancer agent and has shown good anti-leukemic activity in a case of early T-cell progenitor acute lymphoblastic leukemia.
 
BM0026   BMS-986034 ≥98% (HPLC) BMS-986034 is a GPR119 agonist.
 
SML0917   BMS-986122 ≥98% (HPLC) BMS-986122 is a positive allosteric modulator (PAM of the m-opioid receptor). BMS986122 displays little or no agonist activity alone, but dose dependently increases endomorphin-I induced b-arrestin recruitment, and inhibition of forskolin-induced adenyl cyclase activity. The compound also potentiates DAMGO-stimulated GTPgS receptor binding.
 
SML0903   BMS-986124 ≥98% (HPLC) BMS-986124 is a silent allosteric modulator (SAM) of the m-opioid receptor (MOR). The compound BMS-986124 blocks the effects of the MOR positive allosteric modulator BMS-986122, but does not affect binding or activities of orthosteric MOR agonists such as endomorphin-I or DAMGO.
 
BM0021 BMY-14802 ≥97% (HPLC) BMY-14802 is a potent and selective sigma-1 (σ1) receptor antagonist with an IC50 value of approximately 100 nM. BMY-14802 shows low affinity at serotonin (5-HT) 1A and adrenergic σ1 receptors and minimal activity at dopamine receptors. BMY-14802 has exhibited antipsychotic activity in rodent models and anti-dyskinetic effects against L-DOPA with preservation of antiparkinsonian efficacy.
 
BM0032   BMY 45778 ≥98% (HPLC) BMY 45778 is a non-prostanoid prostacyclin agonist.
 
B134 BMY 7378 dihydrochloride ≥98% (HPLC), solid BMY 7378 dihydrochloride is a partial 5-HT1A serotonin receptor agonist and selective α1D-adrenoceptor antagonist.
human ... ADRA1D(146), HTR1A(3350)
SML1838 BNS ≥98% (HPLC) New BNS is a cell penetrant, potent and selective inhibitor of prolyl-hydroxylase 2 (PHD2). BNS regulates ~25% of hypoxia-regulated genes in MCF7 cells.
 
SML0436 BNS-22 ≥98% (HPLC) BNS-22 is a derivative of natural product GUT-70 isolated from the stem bark of Calophyllum brasiliense exhibits antiproliferative activity against human cancer cells. It appears that BNS-22 is a specific DNA-topoisomerase II (TOPO2) catalytic inhibitor. BNS-22 does not induce DNA damage.
 
B8312 BNTX maleate salt hydrate ≥98% (HPLC) BNTX is a selective nonpeptide δ1 opioid receptor antagonist. It antagonizes the effect of D-Pen2,5-enkephalin (a δ1 agonist 4-6 fold, but did not affect the activity of δ2 or μ agonists.<<<107>>> BNTX is used to discriminate among opioid receptor subtypes in effects such as alcohol and drug dependence. It binds 100× more tightly to δ1 than to δ2 receptors. In the tail-flick assay, antinocieceptive ED50 = 646.4 pmol/mouse.
 
B4560 6-Bnz-cAMP sodium salt ≥98% (HPLC) 6-Bnz-cAMP is a membrane permeable and selective cAMP-dependent protein kinase (PKA) activator. For preferential stimulation of cAK type I, a combination with the site B selective analog 8-HA-cAMP or 8-AHA-cAMP can be used.
 
B2682 Boc-Asp(OMe)-fluoromethyl ketone ≥90% (TLC), solid    
B6179 Bongkrekic acid solution from Pseudomonas cocovenenans, ≥95% (HPLC), ~1 mg/mL An antiapoptotic agent, it protects against NMDA receptor induced neuronal apoptosis,­ extends cell survival in cells undergoing apoptosis following infection with viral vectors and abrogates apoptosis induced by hydrogen peroxide in T-cells. It is an inhibitor of adenine nucleotide translocase, which is a component of the mitochondrial permeability transition (MPT) pore complex. Bongkrekic acid prevents mitochondrial depolarization, swelling, rupture of mitochondrial outer membrane, and release of apoptogenic proteins such as cytochrome c. This phenomenon was observed during staurosporine induced apoptosis in Jurkat cells, in HepG2 undergoing apoptosis following TNF-α and ethanol.
 
SML0504   I-BOP ≥95% (HPLC) I-BOP is a potent thromboxane (TP) receptor agonist. I-BOP induces human platelet aggregation with an EC50 value of 0.34 nM.
 
B3061 Borrelidin from Streptomyces parvulus, ≥98% (HPLC) Borrelidin is a potent angiogenesis inhibitor that induces apoptosis in capillary tube-forming cells. Also displays antimalarial activity against drug-resistant Plasmodia. Antimicrobial and selective threonyl t-RNA synthetase inhibitor.
 
SML1265 Bosentan hydrate ≥98% (HPLC) Bosentan is an endothelin receptor antagonist. Endothelin is a potent vasoconstrictor, making antagonists of clinical interest for the treatment of conditions associated with vasospasm, such as subarachnoid hemorrhage (SAH) and hypertension. Bosentan is a dual endothelin receptor antagonist effective in the treatment of pulmonary arterial hypertension (PAH), the first of the class to make it to market. Bosentan is an orally available, competitive antagonist of both the ETA and ETB receptor subtypes with a Ki of 4.7 nM for ETA and a Ki of 95 nM for ETB.
 
PZ0192 Bosutinib ≥98% (HPLC) Bosutinib (SKI-606) is an orally active; dual Src/Abl tyrosine kinase inhibitor with potent antiproliferative activity. It does not appear to inhibit c-Kit and PDGRF, which are thought to be the cause of numerous side effects in anticancer treatment with some other tyrosine kinase inhibitors.
 
B9308 BP897 >98% (HPLC), solid Partially selective D3 dopamine receptor agonist.
human ... DRD2(1813), DRD3(1814), DRD4(1815)
rat ... Adra1a(29412), Adra2a(25083), Drd1a(24316), Drd2(24318), Drd3(29238), Htr1a(24473)
SML1719   BPC 157 trifluoroacetate salt ≥95% (HPLC) BPC 157 is a stable gastric pentadecapeptide that exhibit anti-ulcer and wounds/fistulas healing properties. BPC 157 reduces immediate and delayed damage induced brain trauma and improves nerve regeneration after transection. BPC 157 displays antianxiety and antidepressant effects. It appears that BPC 157 promotes proliferation, migration, and tube formation of human umbilical vein endothelial cells through activation of ERK1/2 phosphorylation.
 
SML0463 BPD ≥98% (HPLC) BPD inhibits LPS-induced NF-kB signaling by inactivation of TAK-1. BPD is also known to inhibit the expression and activity of COX-2.
 
SML0182 bPiDl hydrate ≥98% (HPLC) bPiDI is an α6β2-specific antagonist that inhibits nicotine-evoked and endogenous dopamine release from rat striatal slices (IC50 = 150 nM, Imax = 55%). bPiDI treatment decreases nicotine self-administration, and nicotine-induced locomotor activity in rats.
 
SML0601 BPTES ≥95% (HPLC) BPTES is a selective inhibitor of Glutaminase GLS1 (KGA), which is found in the kidney and brain, and is positively regulated by myc and strongly expressed in many tumors and tumor cell lines. Glutaminase converts glutamine to glutamate, which is an important excitatory neurotransmitter in brain and can be further oxidized to α-ketoglutarate to feed the tricarboxylic acid (TCA) cycle and to glutathione, which is important for controlling the level of reactive oxygen species (ROS), particularly important for cancer cell growth. BPTES was found to slow growth of glioma cells. BPTES is a noncompetitive inhibitor with a Ki of 3 μM.
 
SML0884   bpV(HOpic) ≥90% V basis bpV(OHpic) is a bisperoxovanadium inhibitor of protein phosphotyrosine phosphatases with selectivity for PTEN, phosphatase and tensin homolog, a tumour suppressor phosphatase involved in cell cycle regulation. IC50 values for bpV(HOpic) are 14 nM for PTEN compared to 4.9 μM for PTPβ and 25.3 μM for PTP-1β. bpV(HOpic) has been shown to enhance PI3K/Akt signaling that could prevent myocardium from ischemia-reperfusion injury.
 
SML0889   bpV(phen) ≥95% V basis bpV(phen) is an insulin receptor kinase (IRK) activator and an inhibitor of protein phosphotyrosine phosphatases with selectivity for PTEN, phosphatase and tensin homolog, a tumour suppressor phosphatase involved in cell cycle regulation. IC50 values for bpV(phen) are 38 nM for PTEN compared to 343 nM for PTPβ and 920 nM for PTP-1β. bpV(phen) has anti-inflammatory effects in oxidative stress including inhibitory effects on oxidative stress-induced cardiomyocyte injury that may be partially modulated by the action of ROS on PTEN. It may also be involved in differentiation.
 
SML0885   bpV(pic) ≥95% V basis bpV(pic) is a bisperoxovanadium inhibitor of protein phosphotyrosine phosphatases with selectivity for phosphatase and tensin homolog (PTEN), a tumour suppressor phosphatase involved in cell cycle regulation. IC50 values for bpV(pic) are 31 nM for PTEN compared to 12.7 μM for PTPβ and 61 μM for PTP-1β. bpV(pic) can also act as an insulin mimetic and activate insulin receptor kinase (IRK).
 
SML0497 BQCA ≥98% (HPLC) BQCA is a potent muscarinic M1 receptor positive allosteric modulator with selectivity for M1 over M2-M5. It potentiates M1 activity in in vitro and in vivo assays and is orally bioavailable. Muscarinic 1 (M1) receptors are expressed in brain regions responsible for attention and memory, including hippocampus, cortex, and striatum. BQCA binds allosterically to M1 to enhance the binding and efficacy of ACh at the receptor. 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. BQCA has been shown to improve performance in cognition tasks and increase cerebral blood flow.
 
SML1268   BQU57 ≥98% (HPLC) BQU57 is a selective inhibitor of the Ras-like GTPases RalA and RalB, downstream mediators of Ras signalling, without direct inihibition of Ras or RhoA activity . BQU57 binds to a site on the GDP-bound form of Ral, its inactive state, inhibiting the binding of Ral to its effectors, such as Ral-binding protein 1 (RALBP1; also known as RLIP760, which are involved in proliferation, survival, and metastasis of several human cancers. BQU57 inhibited growth in human luung cancer cell lines with IC50 values of 2.0 μM in H2122 cells and 1.3 μM in H358 cells, and also inihbited tumor xenograft growth.
 
SML0560 BRACO19 hydrochloride ≥96% (HPLC) BRACO19 is a telomerase inhibitor that stabilizes G-quadruplexes, targeting telomeric G-quadruplexes, inducing DNA damage and cell-cycle arrest.
 
SML1406 Brassinazole ≥98% (HPLC) Brassinazole is an inhibitor of the biosynthesis of brassinosteroids, steroid hormones essential for plant growth and development. It has been used to study brassinosteroids function.
 
SML1635 Brassinin ≥98% (HPLC) Brassinin is a phytoalexin isolated from cruciferous vegetables that exhibits anticancer, chemopreventive, antiproliferative and antifungal activities. In lung cancer cells, brassinin inhibits constitutive and IL-6-inducible STAT3 signaling through modulation of PIAS-3 and SOCS-3. It appears that brassinin induces apoptosis in PC-3 prostate cancer cells via the suppression of PI3K/Akt/mTOR/S6K1 signaling.
 
SML1346 BRD32048 ≥98% (HPLC) BRD32048 is a potent inhibitor of ETV1 (ETS variant 1) transcription factor oncoprotein. BRD32048 binds ETV1 directly, modulating both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells.
 
SML1639 BRD3308 ≥98% (HPLC) BRD3308 is a highly selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 value of 65 nM for HDAC3 vs. IC50 values of 1.08 μM and 1.15 μM for HDAC1 and HDAC2, respectively. BRD3308 protected pancreatic β cells, suppressing inflammatory cytokine-induced apoptosis and increasing insulin release without the toxicity associated with HDAC1 and HDAC2 inhibitors. In a rat model of type 2 diabetes, BRD3308 reduced hyperglycemia and increased insulin secretion without affecting weight gain. In another study, BRD3308 was found to activate HIV-1 transcription, disrupting HIV-1 latency.
 
SML1706 BRD4354 ≥98% (HPLC) BRD4354 is a zinc chelating, reversible inhibitor of zinc-dependent histone deacetylases with selectivity for HDAC5 and HDAC9. BRD4354 has IC50 values of 0.85 μM and 1.88 μM for HDAC5 and HDAC9 respectively. Inhibition of other HDACs was lower, with IC50 values of 3.88-13.8 μM for HDACs 4, 6, 7, and 8 and over 40 μM for HDACs 1, 2, and 3. BRD4354′s mechanism is believed to involve zinc-catalyzed decomposition to an ortho-quinone methide, which covalently modifies nucleophilic cysteines within the proteins.
 
SML0567 BRD4770 ≥98% (HPLC) BRD4770 is a selective inhibitor of the histone methyltransferase G9a. BRD4770 blocks lysine residue 9 methylation of histone H3 without inducing apoptosis. In PANC-1 cells, BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway, induces senescence and inhibits anchorage-dependent and -independent growth.
 
SML0813   BRD56491 ≥98% (HPLC) BRD56491 is a nontoxic enhancer of reactive oxygen species (ROS) that strongly elevates markers of oxidative stress without causing cell death. However, combining BRD56491 with nontoxic doses of the glutathione synthesis inhibitor L-buthionine sulfoximine did lead to cell death in a variety of cancer cell lines. BRD56491 can be used to create a more oxidizing cell state and aid in studies of cancer cell lines resilient to induced increases in ROS levels.
 
SML1080 BRD7116 ≥98% (HPLC) BRD7116 is a selective inhibitor of leukemia stem cells. BRD7116 had an EC50 of 200 nM for the leukemia stem cell (LSC)-enriched fraction of cells isolated from the bone marrow of leukemic animals in co-culture compared to ~50% inhibition at 20 μM against normal hematopoietic stem and progenitor cells (HSPCs) and AML cell lines. BRD7116 selectively targeted LSCe cells by cell-autonomous and cell-non-autonomous mechanisms. The exact mechanism is not known, but involved in impairing of the stroma’s ability to support leukemia cells, and inducing transcriptional changes consistent with myeloid differentiation.
 
B7563   BRD7389 ≥98% (HPLC) BRD7398 is a RSK kinase inhibitor that induces insulin expression and differentiation of pancreatic alpha into beta cells. BRD7398 inhibits RSK1, RSK2 and RSK3; IC50 values of 1.5, 2.4 and 1.2 uM, respectively. Treatment of mouse aTC1 cells with BRD7398 induced expression of b-cell markers Pdx1, Pax4, Iapp and Npy and also induced insulin production.
 
SML1361 BRD73954 ≥98% (HPLC) BRD73954 is the first discovered histone deacetylase 6/8 dual inhibitor. BRD73954 has an IC50 of 36 nM for the class IIb HDAC6 and 120 nM for the class I HDAC8 with IC450′s ranging from 9 μM to greater than 33 μM for other HDACs.
 
SML1262 BRD7552 ≥98% (HPLC) BRD7552 is a potent inducer of pancreatic and duodenal homeobox 1 (PDX1) transcription factor that enhanced insulin expression. BRD7552 upregulates PDX1 expression in both primary human islets and ductal cells. It appears that BRD7552 induce PDX1 expression through an epigenetic control.
 
SML1534 I-BRD9 ≥98% (HPLC) I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9), thought to be a member of the chromatin remodelling SWI/SNF BAF complex, which plays a fundamental role in gene expression regulation. I-BRD9 has a pIC50 value of 7.3 with greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7) and greater than 70-fold selectivity against a panel of 34 bromodomains. For full characterization details, please visit the I-BRD9 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML0575 BRD9539 ≥98% (HPLC) BRD9539 is a very specific inhibitor of the enzymatic activity of histone methyltransferase G9a. The compound has poor activity in cell based assays.
 
SML0878   BRD9757 ≥98% (HPLC) BRD9757 is a selective inhbitor of the histone deacetylase HDAC6 (IC50 = 30 nM). BRD9757 dose dependently increases levels of acetylated α-tubulin in HeLa cells, with no affect on H3 acetylation.
 
SML0615   Br-DIF-1 ≥98% (HPLC) Br-DIF-1 is a bromine-substituted derivative of DIF-1 (differentiation-inducing factor-1). Br-DIF-1 significantly increases the efficiency of DMSO-induced differentiation of P19CL6 cells into beating cardiomyocytes by maintaing expression levels of the T-type calcium channel Cav3.1.
 
B7651 Brefeldin A from Penicillium brefeldianum, ≥99% (HPLC and TLC) Brefeldin A (BFA) is a fungal metabolite which disrupts the structure and function of the Golgi apparatus. BFA is an activator of the sphingomyelin cycle. Brefeldin A-mediated apoptosis has been observed in human tumor cells.
Brefeldin A has been shown to increase CRISPR-mediated homology-directed repair (HDR) efficiency.
 
SML0113 Brequinar sodium salt hydrate ≥97% (HPLC) Brequinar exhibits anti-neoplastic activity against refractory solid tumors in human and mouse models. Continuous treatment is required for depletion of pyrimidine pools in the cancer cells and tumor inhibition.
Brequinar inhibits dihydroorotate dehydrogenase (DHODH), the fourth enzyme in the de novo pyrimidine biosynthesis pathway, preventing the synthesis of DNA and RNA. Brequinar has recently been found to have antiviral activity against a broad spectrum of viruses including flaviviruses (dengue virus, West Nile virus, yellow fever virus, and Powassan virus) and also a plus-strand RNA alphavirus (Western equine encephalitis virus) and a negative-strand RNA rhabdovirus (vesicular stomatitis virus).
 
B6434 Bretazenil ≥96% (HPLC), solid Bretazenil is a benzodiazepine partial agonist.
 
SML0216 Brinzolamide ≥98% (HPLC) Brinzolamide is a carbonic anhydrase II inhibitor used to lower intraocular pressure.
 
B169 BRL 37344 sodium salt hydrate solid BRL 37344 is a selective β3-adrenoceptor agonist. Studies support the hypothesis that there are peripheral β3 adrenergic receptors that can reduce food intake and that central β2 or β3 adrenergic receptors mediate the peripheral effects of the β3 agonist.
human ... ADRB3(155)
B4559 BRL 44408 maleate salt ≥98% (HPLC) BRL 44408 maleate is a selective α2A-adrenoceptor antagonist.
 
B0936 BRL 50481 ≥98% (HPLC), solid BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).
human ... PDE7A(5150), PDE7B(27115)
B173 BRL 54443 maleate salt solid Potent 5-HT1E/1F serotonin receptor agonist.
human ... HTR1E(3354), HTR1F(3355)
SML0289 Bromfenac sodium ≥98% (HPLC) Bromfenac is a nonsteroidal anti inflammatory drug (NSAID) that inhibits both COX1 and COX2. It is used as an opthalmic analgesic.
 
B121 Bromoacetylcholine bromide    
B5386 8-Bromoadenosine 3′,5′-cyclic monophosphate ≥97% (HPLC) 8-Bromoadenosine 3′,5′-cyclic monophosphate is a cell-permeable cAMP analog having greater resistance to hydrolysis by phosphodiesterases than cAMP. 8-Bromoadenosine 3′,5′-cyclic monophosphate activates protein kinase A, inhibits growth, decreases proliferation, increases differentiation, and induces apoptosis of cultured cells.
 
B7880 8-Bromoadenosine 3′,5′-cyclic monophosphate sodium salt ≥97% (HPLC), powder Cell-permeable cAMP analog having greater resistance to hydrolysis by phosphodiesterases than cAMP. Activates protein kinase A, inhibits growth, decreases proliferation, increases differentiation, and induces apoptosis of cultured cells.
 
B2432 8-Bromoadenosine-3′,5′-cyclic monophosphorothioate, Rp-isomer ≥98% (HPLC), solid Competitive inhibitor of cyclic AMP-dependent protein kinase A (PKA) type I and II. Membrane-permeable analog of the cAMP inhibitor Rp-cAMPS (Prod. No. A-165).
 
B9392 16β-Bromoandrosterone    
B135 R(+)-6-Bromo-APB hydrobromide solid D1 Dopamine receptor agonist; potent enantiomer.
human ... DRD1(1812)
SML1306 S-p-Bromobenzylglutathione cyclopentyl diester ≥98% (HPLC) S-p-Bromobenzylglutathione cyclopentyl diester (BBGC) is a cell-permeable inhibitor of Glyoxalase 1 (GLO1), an enzyme that detoxifies methylglyoxal, a toxic side-product of glycolysis that induces apoptosis at high levels and has been linked to arterial atherogenesis in diabetics. However, tumors use GLO as well and overexpression of GLO1 has been reported in a number of cancers, so GLO1 inhibitors including BBCG have been investigated as possible anticancer agents. Recent studies have indicated that methylglyoxal has some beneficial effects at low levels with GABAA receptor agonist activity, and that GLO1 inhibition with BBGC can reduce anxiety-like behavior and decrease antiseizure activity. S-p-bromobenzylglutathione cyclopentyl diester should be an inportant tool to study the glyoxalase system.
 
B1552 Bromoenol lactone ≥98% (TLC) Potent, irreversible inhibitor of calcium-independent phospholipase A2 and of magnesium-dependent phosphatidate phosphohydrolase from P388D macrophages (IC50 = 8 μM); enzyme activated irreversible chymotrypsin inhibitor (Ki = 636 nM).
 
B2134 2-Bromo-α-ergocryptine methanesulfonate salt solid Agonist at D2 and D3 dopamine receptors; inhibits prolactin secretion.
human ... DRD2(1813), DRD3(1814), PRL(5617)
B1381 8-Bromoguanosine 3′,5′-cyclic monophosphate sodium salt ≥98% (HPLC), powder Cell-permeable cGMP analog having greater resistance to hydrolysis by phosphodiesterases than cGMP. Activates cGMP-dependent protein kinase. Slows or inhibits the intracellular calcium oscillations of tracheal smooth muscle cells in response to acetylcholine. Reported to mimic the effect of nitric oxide generating drugs.
 
238422 2-Bromohexadecanoic acid ~97% 2-Bromohexadecanoic acid is a PPARδ agonist. It has also been shown to inhibit fatty acid oxidation, inhibit DHHC-mediated palmitoylation, and promote glucose uptake in rat cardiac cells and the insulin-sensitive murine fibroblast line A31-IS.
human ... PPARD(5467)
B2557 8-Bromo-2′-monobutyryladenosine-3′,5′-cyclic monophosphorothioate, Rp-isomer >97% (HPLC), solid    
B3436 N-(4-Bromophenyl)-3-[[(4-bromophenyl)amino]sulfonyl]benzamide ≥98% (HPLC), solid N-(4-Bromophenyl)-3-[[(4-bromophenyl)amino]sulfonyl]benzamide is the first inhibitor of aggregation of the polyglutamine (polyQ) sequence of the Huntington′s Disease protein (huntingtin); polyQ aggregation is neurotoxic, and inhibitors of aggregation may be therapeutic in HD and other polyQ diseases; C2-8 inhibited aggregation in HD PC12 cells with an IC50 of 50nM; when administered in food, suppressed neurodegeneration in vivo in the Drosophila HD model.
 
B6684 Rp-8-Bromo-β-phenyl-1,N2-ethenoguanosine 3′,5′-cyclic monophosphorothioate sodium salt ≥98% (HPLC), powder Rp-8-Br-PET-cGMPS is metabolically stable, competitive inhibitor of cGMP-dependent protein kinase G. Inhibits both PKG I (K= 30 nM) and PKG II and blocks cGMP-gated retinal type ion channels (IC50 = 25 micromoles).
 
SML1078 4-Bromo-Resveratrol ≥98% (HPLC) 4-Bromo-Resveratrol is a resveratrol analog that potently inhibits Sirt1 and Sirt3.
 
SML0992 Bromosporine ≥98% (HPLC) Bromodomains (BRDs) are protein-interaction modules that "read" ε-N-lysine acetylation motifs, such as those found in the N-terminal tails of histones. BRDs have been identified in chromatin-modifying enzymes (such as histone acetyltransferases (HATs)) as well as in transcription factors that regulate genes for cell cycle progression, signal transduction, apoptosis, and inflammation. Proteins containing bromodomains have been implicated in various diseases, such as cancers, inflammatory diseases and neurological diseases. Bromosporine is a broad spectrum BRD inhibitor. In HeLa cells, bromosporine accelerates FRAP recovery of BRD4 and CREBBP at 1μM. For full characterization details, please visit the Bromosporine probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
B9647 (E)-5-(2-Bromovinyl)-2′-deoxyuridine An exceptionally potent inhibitor of Herpes simplex virus type 1.
human ... HV1S(3365)
SML0218 Bropirimine ≥98% (HPLC) Bropirimine is an immunostimulating agent. The compound induces production of α and β interferons and enhances NK cell function. Bropirimine has antiproliferative effects in cancer cell lines and tumor growth in in vivo models.
 
B0378 Brucine sulfate salt hydrate    
SML1868 Brusatol ≥95% (HPLC) New Brusatol (Brutasol) is a plant-derived natural quassinoid that exhibits broad cytotoxicity in cancer cultures (IC50 <1 μM against 457 cancer cell lines) by inhibiting de novo synthesis of cellular proteins (Effective conc. <50 nM in A549 cells), including NRF2.
 
B7431 Bryostatin 1 ≥99%, solid Macrolactone isolated from the marine bryozoan Bugula neritina that initially activates and subsequently down-regulates protein kinase C (PKC). More potent than phorbol myristate acetate for translocating PKCδ and ε.
 
SML1266   Bryostatin 2 ≥95% (HPLC) Bryostatin 2 is potent protein kinase C activator (Ki = 5.9 nM) and an antagonist to phorbol ester tumor promoter 12-0-tetradecanoylphorbol-13-acetate (TPA). Bryostatin 2 exhibits antineoplastic activity against the murine P388 lymphocytic leukemia and human U937 cells.
 
SML1267   Bryostatin 3 ≥95% (HPLC) Bryostatin 3 is a potent protein kinase C activator with a Ki of 2.75 nM, and an antagonist to phorbol ester tumor promoter TPA. Bryostatin 3 is isolated from the bryozoan Bugula neritina.
 
B7937 BSc3094 monohydrobromide ≥98% (HPLC) BSc3094 is a potent inhibitor of tau aggregation and dissolves preformed tau paired helical filaments. BSc3094 interacts closely with the tau protein at the edge involving protons I-IV, while the second attachment site seems to be at the nitro group. In N2A cells (model system for tau aggregation), BSc3094 exhibited low toxicity.