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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.
An orally bioavailable, brain-permeant suppressor of mTOR-mediated autophagy; reduces Aβ levels and prevents cognitive deficits in AβPP/PS1 mouse model.
3-benzyl-5-[(2-nitrophenoxy) methyl]-dihydrofuran-2 (3H)-one (3BDO) blocks rise in LC3-II stimulated by uric acid (UA). It protects the capability of Rheb1-deficient macrophages to perform phagocytosis. 3BDO also prevents the inhibitory effects of EX-527 on eukaryotic translation initiation factor-binding protein 1(4E-BP1) phosphorylation.
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) BAM15 increases mitochondrial respiration rate and is also found to be less cytotoxic compared to other protonophore uncouplers such as carbonyl cyanide p-trifluoromethoxyphenylhydrazone. Hindered oncogenic MAPK (mitogen-activated protein kinase ) signaling leads to BAM15 induced mitochondrial apoptotic pathway activation.
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.
Bovine adrenal medulla 8-22 (BAM8-22), a 15-amino acid peptide, acts a cleavage product of proenkephalin A and the precursor of Leu- and Met-enkephalin in the adrenal medulla. It may also be used to treat pain. It blocks inflammatory pain, chemical pain and downregulates the expression of spinal c-fos gene in an opioid-independent manner. In mice, BAM8-22 diminishes bone cancer pain. It induces the expression of Mas-related G-protein-coupled receptor C (MrgC) in the spinal dorsal horn.
B8684 Bambuterol hydrochloride >98% (HPLC), powder β-adrenoceptor agonist; bronchodilator; anti-asthmatic; terbutaline prodrug
Bambuterol hydrochloride is used for prophylaxis and also to treat chronic bronchitis and chronic asthma in pediatrics.
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.
SML2842 BAY 1125976 ≥98% (HPLC) New BAY 1125976 is an orally active, potent and highly selective AKT1/2 allosteric inhibitor (IC50 = 5.2/18 nM with 10 μM ATP, IC50 = 44/36 nM with 2 mM ATP; AKT3 IC50 = 427 nM with 10 μM ATP) that targets a pocket formed by the kinase & PH domain. BAY 1125976 reduces basal AKT T308/S473 phosphorylation (IC50 = 0.9/1.1; KPL-4 cells) and exhibits anti-cancer efficacy in cultures (IC50 = 0.02-10 μM, 23 human cancer lines) and in xenograft models in vivo (25, 50 mg/kg/day or 5, 15, 25 mg/kg bid. po.; mice), including breast cancers (KPL4 PIK3CAH1074R mutant, MCF7, HBCx-2), AKTE17K-driven prostate cancer LAPC-4, and anal cancer AXF 984.
B5556 Bay 11-7082 ≥98% (HPLC), powder Bay 11-7082 acts as a selective inhibitor for nod-like receptor family pyrin domain containing 3 (NLRP3) inflammasome pathway. In addition, to the inhibition of nuclear factor-kappa B (NF-kB), Bay 11-7082 also triggers apoptosis in anucleated erythrocytes, human T-cell leukemia virus type I (HTLV-I)-infected T-cell lines and primary adult T-cell leukemia cells.
Bay 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation.
B5681 Bay 11-7085 ≥98% (HPLC), solid Bay 11-7085 inactivates peroxisome proliferator-activated receptors γ (PPAR-γ) and increases the microtubule-associated proteins 1A/1B light chain 3B (LC3B), a marker of autophagy resulting in apoptosis in human synovial fibroblasts. It promotes apoptosis in pancreatic carcinoma and may serve as radiotherapy-sensitizing drug. BAY 11-7085 decreases B-cell lymphoma 2 (Bcl-2) by inhibiting pI-κBα (inhibitor of nuclear factor κ B kinase subunit α
Inhibits NF-κB activated expression of ICAM-1, VCAM-1, E-selectin, IL-6 and IL-8.
human ... NFKB1(4790)
SML2817 BAY-1797 ≥98% (HPLC) New BAY-1797 orally available, potent and selective P2X4 antagonist that is suitable for in vivo studies in rodents. BAY-1797 exhibits potent anti-inflammatory and anti-nociceptive effects in mouse CFA inflammatory pain model.
SML2384 BAY 87-2243 ≥98% (HPLC) BAY 87-2243 has a therapeutic effect on ferroptosis‐based cancer, hypoxic pancreatic cancer cells.
BAY 87-2243 is an orally active oxidative phosphorylation (OxPhos) inhibitor that potently suppresses hypoxia-induced HIF-1 activation (IC50 = 0.7 nM by HCT-116-based reporter assay; 24 h 1% O2) by selectively targeting mitochondrial complex I (IC50 = 10 nM using mitochondria from PC3; no inhibition of complex III), exhibiting antiproliferation activity in cancer cultures only in the absence of glucose (IC50 ∼3 nM in H460 cultures with 10 mM galactose or lactate, >10 μM with 10 mM glucose). BAY 87-2243 selectively inhibits hypoxia-induced, but not hypoxia-independent, HIF-1α & HIF-2α upregulation and HIF-1 target genes expression in cultures (IC50 ≤10 nM/ADM, ANGPTL4, CA9 mRNA in H460 cells; IC50 = 2 nM/carbonic anhydrase 9 (CA9) protein in HCT116 cells) and effectively suppresses H460 xenograft tumor growth in mice via daily oral admiminstration in vivo (ED50 ∼2 mg/kg).
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.
SML2281 BAY 60-2770 ≥98% (HPLC) BAY 60-2770 is a potent and selective soluble guanylyl cyclase (sGC) heme-independent activator that protects sGC from heme oxidation in smooth muscle tissues. BAY 60-2770 provides cardioprotection and limits the infarct size in rat ischaemia-reperfusion model. Also BAY 60-2770 Ameliorates of urethra dysfunction in high-fat fed obese mice.
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.

BAY-364 (BAY-299N) is the negative control for the active, structurally similar probe, BAY-299. BAY-364 is available from Sigma. To learn more about and purchase BAY-364, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
B9685 BAY 61-3606 hydrochloride hydrate ≥98% (HPLC), powder BAY 61-3606 helps to prevent the degranulation of freshly isolated basophils. It also prevents B cell receptor (BCR)-mediated signaling.
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).
SML1783 BAY-364 ≥98% (HPLC) BAY-364 (BAY-299N) is structurally similar to selective BRD1/TAF1 inhibitor BAY-299 and serves as inactive control. BAY-364 is inactive against BRD1 and exhibit moderate activity against TAF1 (3 μM). For full characterization details of the active probe, please visit the BAY-299 probe summary on the Structural Genomics Consortium (SGC) website.

BAY-299, the active probe, is available from Sigma. To learn more about and purchase BAY-299, click here.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
SML2444 BAY 41-4109 ≥98% (HPLC) BAY41-4109 is a heteroaryldihydropyrimidine (HAP)-based capsid assembly modulator (CAM) that destabilizes hepatitis B virus (HBV) capsid assembly. BAY41-4109 inhibits HBV replication in HepG2.2.15 cultures with little host cytotoxicity (IC50 = 53 nM vs. CC50 = 7 μM in 8 days). Despite its relatively short half-life in vivo (plasma t1/2 = 5 h/dog, 2 h/rat, ≤1 h/mouse), BAY41-4109 shows greater antiviral efficacy than 3TC in Tg [HBV1.3 fsX-3′5′] mice (HBV DNA reduction = 52%/BAY vs. 36%/3TC in liver via 30 mg/kg b.i.d. p.o.; 70% vs. 30% in plasma with 15 mg BAY/kg or 30 mg/kg 3TC b.i.d. p.o., respectively) with good oral availability (F/tmax =31%/mouse, 58%/rat & dog).
SML1780 BAY-588 ≥98% (HPLC) BAY-588 is an inactive control probe for BAY-876. 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.

BAY-876, the active GLUT1 probe, is available from Sigma. To learn more about and purchase BAY-876, click here.

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.

BAY-369 is the negative control for the active probe, BAY-598. To request a sample of the negative control from the SGC, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML2325 BAY-6035 ≥98% (HPLC) BAY-6035 is a substrate-competitive, potent and selective SMYD3 inhibitor (IC50 = 88 nM by cell-free MEKK2 peptide methylation; IC50 = 70 nM against cellular MEKK2 methylation) with >100-fold selectivity over other histone methyltransferases. BAY-211 is a structural analog and the recommended inactive control (IC50 = 23 μM by cell-free MEKK2 peptide methylation) for BAY-6035. For characterization details of BAY-6035, please visit the BAY-6035 probe summary on the Structural Genomics Consortium (SGC) website.

BAY-444 is the negative control for the active probe, BAY-6035. To request a sample of the negative control from the SGC, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML2349 BAY-604 ≥97% (HPLC) BAY-604 is a control probe for BAY-707, an inhibitor of the human 7,8-dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1)
SML1958 BAY 60-6583 ≥98% (HPLC) BAY 60-6583 is a potent adenosine receptor A2b (A2bR) partial agonist (Ki against 0.3 nM [3H]PSB-603 for binding human/mouse/rat A2bR = 114/136/100 nM) that selectively induces cAMP-dependent transcription activity in CHO transfectants expressing human A2bR (EC50 ~100 nM), but not A1R or A2aR, while exhibiting no affinity toward human/rat/mouse A2aR. BAY 60-6583 also displays low-affinity antagonistic activity toward A1R (Ki against 1 nM [3H]CCPA for binding human/mouse/rat A1R = 387/351/514 nM; IC50 = 7.4 μM against 100 nM CCPA-induced hA1R β-arrestin recruitment) and A3R (Ki against 10 nM [3H]NECA for binding human/mouse/rat A3R = 223/3920/2750 nM; IC50 = 6.7 μM against 30 nM Cl-IB-MECA-induced hA3R β-arrestin recruitment). BAY 60-6583 is widely administered in animals in vivo via i.p. (0.1-80 mg/kg) or i.v. (0.2-2 mg/kg) for studying A2bR-mediated biological responses.
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, 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.

BAY-678, the active HNE probe, is available from Sigma. To learn more about and purchase BAY-678, click here.

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.

BAY-677 is used as a negative control and is available from Sigma. To learn more about and purchase BAY-677, click here.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
SML2348 BAY-707 ≥98% (HPLC) BAY-707 is an inhibitor of the human 7,8-dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1), which hydrolyzes oxidized purine nucleoside triphosphates that might otherwise be incorporated into DNA/RNA and contribute to DNA damage. BAY-707 was shown to be a substrate-competitive, selective MTH1 inhibitor with an IC50 value of 2.3 nM.
SML2311 BAY 60-7550 ≥95% (HPLC) BAY 60-7550 is an orally active, potent and selective cGMP-dependent phosphodiesterase PDE2 (PDE2A) inhibitor (human/bovine PDE2 IC50 = 4.7/2.0 nM; bovine PDE1 IC50 = 108 nM, human PDE5/5A/10A/4B IC50 = 240/580/704/940/1830 nM, human PDE3B/7B/8A/9A/11A IC50 >4 μM) with little activity (IC50 >10 μM) toward acetylcholinesterase, mAO-A/B, adenosine deaminase, and many receptor subtypes tested. Bay 60-7550 effectively upregulates cGMP and cAMP level in cultured rat and murine neurons (1 nM-1 μM) exposed to guanylyl cyclase (GC) or adenylyl cyclase (AC) stimulator (1 μM Bay 41-8543 or 2 μM forskolin), respectively, as well as exhibits learning and memory-improving efficacy in rats (0.6-3 mg/kg p.o.) and mice (0.3-1 mg/kg p.o.) in vivo.
SML2670 BAY-8002 ≥98% (HPLC) BAY-8002 is an orally available, potent and selective inhibitor of lactate transporter MCT1 (monocarboxylate transporter 1; SLC16A1) that potently inhibits bidirectional lactate transport. BAY-8002 exhibits antiproliferative activity in numerous cancer cell lines. BAY-8002 induces accumulation of lactate and significantly inhibits tumor growth in mice model. It does not cause tumor regression.
SML2727 BAY 41-8543 ≥98% (HPLC) BAY 41-8543 is a stimulator of soluble Guanylyl cyclase (guanylate cyclase, sGC), the primary cellular receptor for nitric oxide (NO).
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.

BAY-588 is the negative control for the active probe, BAY-876. BAY-588 is available from Sigma. To learn more about and purchase BAY-588, click here.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
SML2604 BAY-885 ≥98% (HPLC) BAY-885 is an ATP site-targeting, potent and selective ERK5 (BMK1, MAPK7) inhibitor (IC50 = 35 nM with 250 μM ATP; % inhibition at 1 μM = 62/rat Fer, 58/human EphB3, 43/human EphA5, =20/355 kinases) with no BRD4 affinity (20 μM), nor inhibitory potency toward hERG (10 μM) and CYP enzymes (20 μM; CYP1A2, CYP2C8, CYP2C9, CYP2D6, CYP3A4). BAY-885 potently inhibits 100 ng/mL EGF-induced, ERK5-dependent MEF2 activity (IC50 = 120 nM; SN12C-MEF2-luc reporter assay).
SML2436 BAY-958 hydrochloride ≥98% (HPLC) BAY-958 (LDC526) is an orally active, ATP site-targeting, potent and selective PTEFb/CDK9 inhibitor (hCDK9-CycT1 IC50 = 5-11 nM; [ATP] = 10 μM) with 52- to >2000-fold selectivity over CDK1-7 with antiproliferative activity in cancer cultures (IC50 = 0.28 μM/96h/MOLM-13, 1 μM/96h/HeLa, 0.55 μM/48h/MEC-1, 0.28 μM/48h/CCL patient PBMCs). When administered orally in mice, BAY-958 significantly suppresses MOLM-13 acute myeloid leukemia (AML) tumor growth in mice (30/40 mg/kg/day p.o.; HCl salt) and exhibits in vivo efficacy in two murine chronic lymphocytic leukemia (CLL) models (50 & 70 mg/kg/day p.o.; free base).
B133 (S)-(−)-Bay K8644 ≥98% (HPLC), solid (S)-(-)-Bay K8644 enhances Ca2+ current, whereas the (+)-Bay K 8644 is a weak Ca2+ channel antagonist. Bay K 8644 is lipophilic and it effectively scavenges superoxide anions.
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.
SML2250 BB-Cl-amidine trifluoroacetate salt ≥98% (HPLC) BB-Cl-amidine is an irreversible pan-protein-arginine deiminase (PAD) inhibitor (kinact/KI in M-1min-1 = 16100/PAD1, 4100/PAD2, 6800/PAD3, 13300/PAD4) with >20-fold increased potency against U2OS osteosarcoma cutlures (viability assay IC50 = 8.8 μM vs >200 μM with Cl-amidine) and longer in vivo half-life (1.75 hrs vs 15 min for Cl-amidine in plasma post injection in mice) than Cl-amidine. BB-Cl-amidine effectively inhibits PMA-induced neutrophils extracellular trap (NET) formation from lupus-prone MRL/lpr mice-derived bone marrow neutrophils in cultures (by 78% and 34% with 20 μM BB-Cl-amidine or Cl-amidine, respectively), while daily s.c. injection (1 mg/kg) is efficacious in ameliorating lupus symptoms in in MRL/lpr mice in vivo.
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 has the ability to block PDE8A (phosphodiesterase 8A) and PDE4A (phosphodiesterase 4A) with IC50 values of 280 and 220 nM. It helps to increase the synthesis of the steroid from both primary Leydig cells and MA-10 cells.
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).
BCI121 is capable of reducing the mesenchymal signature of MDA-MB-231 cells. It can also decrease their ability to invade in vitro and in vivo.
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.
SML2226 BC-LI-0186 ≥98% (HPLC) BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM) without affecting LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 inhibits Leu-dependent LRS lysosomal membrane localization (10 μM), RagD GTPase and mTORC1 activation (IC50 = 81.4 nM against Leu-induced S6K phosphorylation), but not ARF1 activation, AKT S473 phosphorylation, Glu- or Arg-dependent S6K phosphorylation, nor the cytosolic and mitochondrial LRS catalytic activities. BC-LI-0186 effectively suppresses the growth of rapamycin-resistant MCT116 MM cancer cells with mTOR-S2035I mutation both in cultures (GI50 = 42.03) and in mice in vivo (by 40% in 2 wks; 20 mg/kg/day i.p.).
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.
SML2328 BD064 ≥98% (HPLC) BD064 is a probe-dependent and biased negative allosteric modulator (NAM) of the chemokine receptor CXCR3 signaling that preferentially inhibits CXCL11-mediated ?-arrestin 2 recruitment over G protein activation.
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.
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.
In native tissues, 5-BDBD is considered as a beneficial antagonist to analyze the effect of P2X receptors (P2XRs) subtype P2X4R.
SML2639 BDT001 ≥98% (HPLC) BDT001 is a selective negative allosteric modulator of Flt-3 receptor tyrosine kinase. It showed minimal binding to 25 diverse RTKs and 49 intracellular kinases. In primary cultures of adult DRG neurons, BDT001 reversed the potentiation of capsaicin-induced TRPV1 activation by FL, with a maximal effect at 1 μM. In a mouse study BDT001 alleviated nerve injury-induced peripheral neuropathic pain but had no effect on nociception in non-injured animals.
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.
BEC is a boronic analog of L-arginine, and L-cysteine. It competitively inhibits both arginase I and II. BEC does not directly affect nitric oxide synthase.
B0385 Beclomethasone ≥99% Beclomethasone is an anti-inflammatory glucocorticoid.
It helps to decrease airway hyperresponsiveness. It also helps to regulate symptoms of asthma.
human ... CYP1A2(1544)
SML2209 Benactyzine hydrochloride ≥98% (HPLC) Benactyzine is an anticholinergic and antimuscarinic drug that was used as antidepressant. Benactyzine was discontinued in US due to its ineffectiveness.
B0935 Benazepril hydrochloride ≥98% (HPLC), solid Benazepril is a long-acting angiotensin converting enzyme (ACE) inhibitor.
human ... ACE(1636)
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.
Bendamustine is a therapeutic agent employed in treating lymphomas and chronic lymphocytic leukemia. It may be useful in central nervous system (CNS) malignancies treatment regimen due to its penetration capacity into brain tissue. Bendamustine is a promising candidate for non-Hodgkin lymphoma and Hodgkin lymphoma therapies.
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 Benserazide can block HK2 enzymatic activity in vitro. It is used along with levodopa to treat Parkinson′s disease.
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.
human ... SLC18A2(6571)
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.
Benztropine mesylate serves as an inhibitor of breast cancer stem cells (BCSCs) in vitro and in vivo. It can help in improving the efficacy of chemotherapy in vitro. It is considered as an anti-cancer stem cell (CSC) drug, which can modify tumorigenic properties.
human ... CHRM1(1128)
UC440 Benzydamine N-oxide hydrogen maleate CYP2C9 substrate
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.
O6-Benzylguanine (O6BG) inhibits methylguanine methyltransferase (MGMT) by blocking the active site through benzyl group transfer. The use of O6BG with bis-chloroethylnitrosourea (BCNU) or carmustine is effective in treating solid tumors including lymphomas, melanomas and sarcoma.
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.
SML2616 Bepotastine besilate ≥98% (HPLC) Bepotastine besilate is a second generation antihistamine used clinically for the treatment of itching associated with allergic conjunctivitis, allergic rhinitis and urticaria/pruritus. It is a direct H1-receptor antagonist that inhibits the release of histamine from mast cells.
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.
human ... CACNA1A(773), CACNA1B(774), CACNA1C(775), CACNA1D(776), CACNA1E(777), CACNA1F(778), CACNA1G(8913), CACNA1H(8912), CACNA1I(8911), CACNA1S(779), CACNA2D1(781), CACNA2D2(9254), CACNA2D3(55799), CACNA2D4(93589), CACNB1(782), CACNB2(783), CACNB3(784), CACNB4(785), CACNG1(786), CACNG2(10369), CACNG3(10368), CACNG4(27092), CACNG5(27091), CACNG6(59285), CACNG7(59284), CACNG8(59283)
SML2164 Bepristat 1a ≥98% (HPLC) Bepristat 1a 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 1a binds at the substrate-binding site, rather than the catalytic site. It blocked PDI activity with an IC50 value of 700 nM. PDI is up-regulated in several cancers, has been implicated in neurodegenerative processes, and plays an important role in thrombus formation. Bepristat 1a potently inhibited platelet aggregation and thrombus formation in vivo.
SML1925 Bepristat 2a hydrochloride ≥95% (HPLC) 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.
Beraprost sodium is used as a therapeutic agent for chronic artery obstructions or primary pulmonary hypertension. In individuals with coronary artery disease, beraprost sodium helps to reduce oxidative stress and developed forearm endothelium dependent vasodilation.
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.
Besifloxacin is a broad spectrum fourth-generation fluoroquinolone antibiotic.
Besifloxacin stops the production of pro-inflammatory cytokines in vitro.
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% Betamethasone, an isomer of dexamethasone is also termed as 9α-fluoro-16β-methyl-11 β,17,21-trihydroxypregna-1,4-dien-3,20-dione or 9α-fluoro-16β-methylprednisolone (27.1.52). It can be used as an anti-itch agent and treating dermatitis and eczema.
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% Betamethasone is used to treat neonatal respiratory distress syndrome, and psoriasis.
human ... NR3C1(2908)
B0515 Betamethasone 17-valerate Betamethasone 17-valerate is a synthetic glucocorticoid. It exhibitstherapeutic effects against various allergic and inflammatory skin diseases. Betamethasone 17-valerate also possesses anti-inflammatory properties.
B5683 Betaxolol hydrochloride >98% (HPLC) Betaxolol hydrochloride has the ability to block calcium channels. Betaxolol is a selective β1 adrenoreceptor antagonist. It has neuroprotective effects on retinal neurons.
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).
BetP is a trimeric Na+-coupled betaine symporter. BetP belongs to the betaine-choline-carnitine transporter (BCCT) family. It controls transport activity in dependence of the cytoplasmic K+-concentration.
SML2845 Betrixaban ≥98% (HPLC) New Betrixaban is an orally active, active site-targeting, highly potent and selective factor Xa (fXa) inhibitor (IC50 = 1.5 nM; Ki = 117 pM) with much reduced plasma kallikrein inhibitory activity (IC50 = 6.3 μM) and little potency against thrombin, trypsin, t-PA, aPC or plasmin inhibition (IC50 >10 μM). Betrixaban exhibits good pharmacokinetic properties and anticoagulant efficacy against various thromboembolism (VTE) events in vivo.
SML2057 Bevirimat ≥98% (HPLC) Bevirimat is the first in class HIV maturation inhibitor. It acts by inhibiting the processing of the Gag capsid (CA)/spacer peptide 1 (SP1), which causes accumulation of CA/SP1 (p25) precursor proteins and blocks maturation of the viral core particle.
It also causes defective core condensation and releases the non-infectious virus particles from cells infected with human immunodeficiency virus (HIV). Thus, bevirimat blocks the spread of HIV infection to other cells.
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.
Bexarotene is used to treat breast cancer.
human ... RXRA(6256), RXRB(6257), RXRG(6258)
B7273 Bezafibrate ≥98%, solid Bezafibrate has the ability to repress HCV assembly and secretion. It is used to treat dyslipidemia.
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.
SML2214 BI01383298 ≥98% (HPLC) BI01383298 is a selective probe for the Na(+)/citrate co-transporter (NaCT), SLC13A5. For characterization details of BI01383298, please visit the BI01383298 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes, visit sigma.com/sgc
SML2255 BI-2545 ≥98% (HPLC) BI-2545 is a PF-8380 structure analog with improved autotaxin (ATX; ENPP2) inhibitory potency (human/rat ATX IC50 = 2.2/3.4 nM, IC50 = 29/96 nM using human/rat whole blood (WB); human ATX/rat ATX/rat WB IC50 = 6.5/13/307 nM with PF-8380), in vivo pharmacokinetic profile, oral availability, and lysophosphatidic acid (LPA)-lowering efficacy (BI-2545 Cmax/AUC/T1/2/Max 18:2 LPA reduction = 140 nM/675 nM•h/3.4 h/90.4% post 10 mg/kg p.o. in rats vs. 60.3 nM/342 nM•h/2.5 h/32.2% with PF-8380). BI-2545 exhibits no hERG inhibitory activity (IC50 >10 μM vs. 480 nM with PF-8380) and displays significant cross-reactivity towards only 4 targets among a panel of 48 enzymes/receptors/transporters/channel proteins at a high concentration of 10 μM (55%, 80%, 66%, 61% inhibtion of 5-HT2a, L-type Calcium channel, Na+ channel site 2, and norepinephrine transporter, respectively).
B0186 BI-6C9 ≥97% (HPLC), solid BI-6C9 is a tBid inhibitor and antiapoptotic.
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.
SML2481 BI-9321 Hydrochloride ≥98% (HPLC) BI-9321 is a highly selective and potent inhibitor of histone lysine methyltransferase NSD3 PWWP-1 domain that binds to methylated Lysine residue.
SML1655 BI-9564 ≥97% (HPLC) BI-9564 decreases the development of tumors and enhances the survival rate in treated mice. It can block BRD9 (bromodomain-containing protein 9) and BRD7 (bromodomain-containing protein 7). BI-9564 is sevenfold more effective on BRD9 and fourfold more effective on BRD7.
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.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
rat ... Scnn1g(24768)
SML0306 Biapenem ≥98% (HPLC) Biapenem does not react to renal dihydropeptidase-I mediated hydrolysis in human. Biapenem is well absorbed by tissues and body fluids, following intravenous injection.
Biapenem is a broad spectrum, carbapenem-based antibiotic with activity against both Gram-positive and Gram-negative bacterial strains.
SML2426 BIBN4096BS ≥95% (HPLC) BIBN4096BS (Olcegepant) is a potent calcitonin gene-related peptide (CGRP) receptor antagonist with higher affinity/potency toward human over rat & mouse receptor (human/rat Ki = 14.4 pM/3.4 nM by binding assay; human/mouse Kb = 8 pM//7.711 nM by cellular cAMP assay). BIBN4096BS inhibits facial blood flow by electrical stimulation of marmoset monkey trigeminal ganglion (IC50 = 3 μg/kg i.v.) without any intrinsic cardiovascular effects. Studies using anaesthetized rats reveals that BIBN4096BS antagonism against trigeminal nociceptive stimulation by capsaicin is limited to the spinal trigeminal nucleus, but not trigeminal ganglion. Also widely employed for in vivo studies in mice.
SML2094 BIBO 3304 trifluoroacetate salt ≥98% (HPLC) BIBO 3304 is a highly potent and selective NPY Y1 receptor antagonist that inhibits food intake induces by NPY (neuropeptide Y) or fasting in rodents. BIBO3304 eliminates NPY effects on fear extinction retrieval in rats.
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.
human ... AR(367)
B8435 BiCAPPA ≥97% (HPLC), solid Inhibitor of the formation of abnormal ß-rich isoform of prion protein PrPSc.
14340 (+)-Bicuculline ≥97.0% (TLC) (+)-Bicuculline acts as a competitive inhibitor of GABA liganding binding to the receptor.
(+)-Bicuculline is a GABAA receptor antagonist.
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.
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.
human ... DRD2(1813), HTR1A(3350)
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.
Bifonazole is used to treat several infections such as onychomycoses, otomycoses, erythrasma, psoriasis, sebopsoriasis, seborrhoeic dermatitis and rosacea. Bifonazole is also used as an important drug to treat melanoma.
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.
SML2450 BIIE 0246 hydrochloride ≥98% (HPLC) BIIE0246 is a high-affinity, competitive non-peptide antagonist for the neuropeptide Y (NPY) Y2 receptor (Ki = 8-15 nM). BIIE0246 potently blocks NPY effects in rat hippocampus.
SML2286 BIIL260 hydrochloride ≥98% (HPLC) BIIL260 is a selective and potent leukotriene B4 (BLT1) receptor antagonist with a Ki value of 1.8 nM in human U937 cells. BIIL260 was used found to act as an inverse agonist, stabilizing the inactive state of BLT1.
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 Highly selective k-opioid receptor antagonist. nor-Binaltorphimine has antidepressant properties.
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.
SML2555 BIO-0919278 racemate ≥98% (HPLC) BIO-0919278 is a highly selective cyclin-dependent kinase CDK12 inhibitor (Kd = 5.6 μM) with little or no potency against CDK1-7, CDK9, CDK14, CDK16-18 or 344 other kinases (<35% inhibition at 1 μM). BIO-0919278 reduces CDK12-mediated Pol II CTD Ser2 phosphorylation (by 57% at 1 μM; U-2 OS cells) without affecting CDK12-independent Pol II CTD Ser5 phosphorylation, and selectively targets noncanonical NF-κB activation (4-hr 20 ng/mLTWEAK-induced p52 nuclear translocation/NIK mRNA production IC50 = 167/320 nM; U-2 OS cells) without affecting canonical NF-κB activation (TNF-α-stimulated p65 (RelA) nuclear translocation IC50 >30 μM).
SML2497 BIO 1211 trifluoroacetate salt ≥97% (HPLC) BIO 1211 is a selective, tight-binding α4β1 (VLA-4, very late antigen-4; koff = 1.4 x 10-4/s, KD = 70 pM) integrin antagonist (VCAM-Ig Jurkat surface binding IC50 = 1 nM; integrin-mediated cell adhesion IC50 = 4 nM/α4β1, 2 μM/α4β7, >100 μM/α1β1, α5β1, α6β1, αLβ2, αIIBβ3) based on the Leu-Asp-Val (LDV) sequence from the alternatively spliced connecting segment-1 (CS-1) of fibronectin (aa 1980-1983). In addition to probing α4β1-mediated cellular responses, BIO 1211 is also widely used in animal disease models in vivo, including MS (5-10 mg/kg; murine EAE) and asthma (1-10 mg/kg via intranasal or nebulizer to mice, rats, sheep; 3 mg/sheep iv.).
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.
SML2135 Biotinyl tyramide ≥97% (HPLC) Biotinyl tyramide is a reagent used for tyramide signal amplification for both immunohistochemistry (IHC) and in situ hybridiztion protocols and with either chromogenic or fluorescence detection. Preliminary binding of a probe is followed by secondary detection of the probe with an HRP-labeled antibody or streptavidin conjugate. Catalysis by the HRP results in the deposition of multiple biotinyl tyramide molecules in the immediate vicinity of the probe that can then be detected with a labeled streptavidin conjugate. Detection sensitivity can be 100-fold or more sensitive compared to conventional detetion procedures.
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.
human ... CHRM1(1128)
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% 3,3-Bis(aminoethyl)-1-hydroxy-2-oxo-1-triazene is a long-acting nitric oxide donor. It might exhibit nociceptive effects in rats.
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.
Bisantrene is an anthracene bishydrazone derivative, which has antitumor activity.
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) 6,8-Bis(benzylthio)-octanoic acid is an E1α pyruvate dehydrogenase (PDH) modulator that prevents cancer cells from metabolizing glucose for energy. 6,8-Bis(benzylthio)-octanoic acid 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.
Bisdemethoxycurcumin (BMDC) is a stable dimethoxy derivative of curcumin and is useful as a supplement in cell culture medium. It also possesses antimicrobial, antioxidative and neuroprotective functionality.
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 Bisoprolol hemifumarate is useful in oral formulations due to its high bioavailability. It also shows long elimination half-life.
Cardioselective β1-adrenoceptor antagonist.
human ... ADRB1(153)
D3415 Bisphenol A diglycidyl ether PPARγ inhibitor that blocks rosiglitazone- and insulin-induced adipogenesis.
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.
Bivalirudin trifluoroacetate salt is a synthetic peptide composed of 20 amino acids. It serves as an anticoagulant for patients with unstable angina undergoing coronary angioplasty.
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.
SML2355 BIX02189 ≥98% (HPLC) BIX02189 is an ATP site-targeting, potent and selective MEK5 inhibitor (IC50 =1.5 nM, [ATP] = 750 nM) with much reduced or no potency against 79 other kinases (CSF1R (FMS)/ERK5/Lck/Jak3/TGFβR1/RPS6KA6 (RSK4) IC50 = 46/59/250/440/580/990 nM, MEK1/MEK2/ERK2/JNK2/EGFR/STK16 IC50 >6.2 μM). BIX02189 blocks cellular ERK5, but not ERK1/2 or p38, phosphorylation induction (IC50 <1 μM in sorbitol-stimulated HeLa), as well as downstream MEF2C transcriptional activation (IC50 = 0.53/0.26 μM, MEK5/ERK5/MEF2C HeLa/HEK293 reporter cells). BIX02189 in vivo efficacies are demonstrated in murine models of atherosclerosis, cancer, and diabetes (10-20 mg/kg i.p.).
B2186 BL-1249 ≥98% (HPLC) BL-1249 also activates TWIK related potassium channel 2 (TREK2). It interacts with K2P channel at the negatively charged activator site and modulates channel opening.
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 U/mg 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 has the ability to bind ribosomal DNA and prevent RNA polymerase I (Pol I) transcription and results in the disintegration of the nucleolus. It does not impair DNA damage detection. BMH-21 is considered as an important activator of the p53 pathway.
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.
BML-210 is a synthetic benzamide and is a potential tumor inhibitor. It is used as a therapeutic agent to treat promyelocytic leukemia. In human leukemia cell lines (NB4, HL-60, THP-1, and K562), BML-210 modulates histone deacetylase and promotes apoptosis. BML-210 favors frataxin expression in neurodegenerative disease Friedreich′s ataxia (FRDA). It interacts with myocyte enhancer factor-2 (MEF2) via hydrogen-bonding and prevents histone deacetylase 4 (HDAC4) binding.
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.
BMS-189453 specifically has sufficient bioavailability in rats and monkeys. BMS-189453 only binds to α, β, and γ retinoid receptors but its activation is unknown. BMS-189453 is found to inhibit the action of collagenase-3 (MMP-13) which catalyses cartilage matrix degradation. Thus, it serves to treat rheumatoid arthritis.
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.
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-191264 decreases cardiac necrosis and improves the recovery of contractile activities after reperfusion.
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 (MaxiPost [(3S)-(+)-(5-chloro-2-methoxyphenyl)-1,3-dihydro-3-fluoro-6-(trifluoromethyl)-2H-indole-2-one)] is used to treat ischemic stroke. It also acts as an activator of KNCQ4 (KQT-like subfamily, member 4) and KCNQ5 (KQT-like subfamily, member 5) with equal potency.
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.
human ... KCNMA1(3778), KCNQ2(3785), KCNQ3(3786), KCNQ4(9132), KCNQ5(56479)
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.
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.
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.
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.
human ... EGFR(1956), ERBB2(2064), ERBB4(2066)
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.
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).
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.
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) 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.
SML2611 Bobcat339 ≥98% (HPLC) Bobcat339 is a cell penetrant, potent and selective inhibitor of TET1 and TET2 [Ten-eleven translocation methylcytosine dioxygenase (TET) 1 and 2] that reduces content of 5-hydroxymethyl-cytosine (5hmC) in cultured neurons. Bobcat339 does not inhibit DNMT3a.
B2682 Boc-Asp(OMe)-fluoromethyl ketone ≥90% (TLC), solid Boc-Asp(OMe)-fluoromethyl ketone (Boc-D-fmk) permits cell permeability. It is a caspase inhibitor and suppresses apoptosis induced by various kinds of stimuli. Boc-D-fmk poorly inhibits caspases-2, -5, -6 and -10.
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.
SML1994   BOP >97% (HPLC) BOP (N-(Benzenesulfonyl)-L-prolyl-L-O-(1-pyrrolidinylcarbonyl)tyrosine sodium salt) is a potent and selective dual inhibitor of integrins alpha-4 beta-1 (α4β1) and alpha-9 beta-1 (α9β1) with Kd values in the picomolar range. BOP has been shown to preferentially mobilize hematopoietic stem cells (HSCs) and progenitors and to act synergistically with AMD3100.
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.
Bosentan is found to decrease deposition of collagen in the lungs, which has been observed in bleomycin-induced pulmonary fibrosis rat model.
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.
human ... ABL1(25), HCK(3055), LYN(4067), SRC(6714)
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 gut peptide and possesses free radical scavenging activity. This peptide stimulates nitric oxide synthase generation and therefore offers gastric cytoprotection. Unlike other peptides, BPC 157 is effective without a carrier. It participates in muscle healing and is used in the treatment of gastrocnemius muscle complex.
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.
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.
SML2305 BPK-29 ≥98% (HPLC) BPK-29 is a potent and selective NR0B1 ligand that covalently binds to NR0B1 Cys 274. BPK-29 inhibits the NR0B1-SNW1 interaction. It inhibits the anchorage-independent growth of KEAP1-mutant cancer cells.
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.
Vaccinia virus (VACV) requires glutamine metabolism for its optimal replication. Inhibition of glutaminolysis by bis-2-(5-phenylacetamido-1,3,4-thiadiazol-2-yl)ethyl sulfide (BPTES) can be a potential method to treat poxvirus infections.
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) (potassium bisperoxo(bipyridine)oxovanadate) shows protective effect against disease progression in leishmaniasis by mediating NO-dependent microbicidal action.
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) contains a polar side chain, and specifically inhibits PTEN(phosphatase and tensin homolog) unlike its parent compound, which targets several other phosphatases too. Thus, making bpV(pic) more a prefered inhibitor. bpV(pic) is recognized as a potent activator of multiple sclerosis (an autoimmune disorder) related human endogenous retroviruses.
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.
Telomerase is associated with tumor progression and is highly expressed in a number of tumors. BRACO19 is known to prevent the capping and catalytic action of telomerase and thus, might serve as an effective therapeutic approach for cancer treatment. BRACO19 establishes antiviral activity against HIV (human immunodeficiency virus).
SML2606 Bragsin2 ≥98% (HPLC) Bragsin2 is a hydration resistant cell penetrant, potent and selective noncompetitive inhibitor of ArfGEF BRAG2 (Afr guanine nucleotide exchange factor BRAG2) that inhibits Arf GTPase activation in vitro and in cells. It binds to pleckstrin homology (PH) domain of BRAG2 and misposition BRAG2 on the membrane. Bragsin2 disrupt the function of the yeast ArfGEF Sec7p. Bragsin2 suppresses tumorsphere formation of some breast cancer stem cell lines including SUM149 and S68.
SML1406 Brassinazole ≥98% (HPLC) Brassinazole induces dwarfism and morphological changes in Arabidopsis, which results in similarity with brassinosteroid deficient mutants. These changes were neutralized by brassinolide treatment, indicating that brassinazole leads to brassinolide deficiency in Arabidopsis.
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.
SML2132 Brazilin Brazilin is a natural isoflavonoid red pigment with many biologic activities including neuroprotective, anti-inflammatory, antibacterial, antiproliferative, and antioxidant properties. Some of its activity is thought to be due to its regulation of the transcription factor NF-ΚB.
SML1346 BRD32048 ≥98% (HPLC) BRD32048 is a derivative of [1,3,5]triazine. It is found in orally active phosphodiesterase inhibitors (PDE) inhibitors, DHFR (dihydrofolate reductase) inhibitors and phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors. BRD32048 binds ETS variant 1 (ETV1) and controls transcriptional activity, facilitated by ETV1 and invasion of ETV1-driven cancer cells.
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.
BRD3308 promotes outgrowth of HIV-1 (human immunodeficiency virus 1) from inactive infected patient cells. It helps to increase β-cell proliferation.
SML1706 BRD4354 ≥98% (HPLC)