bms-3

BMS-3 is a potent LIMK inhibitor with IC50 values of 5 nM and 6 nM for LIMK1 and LIMK2, respectively.

VU0652925 is a PAR4 antagonist. VU0652925 has a P-sel IC50 of 39.2 pM (-pIC50±SEM: 10.41±0.04) and a PAC1 IC50 of 43.0 pM (-pIC50±SEM: 10.4±0.04).

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

BMS817378 is a potent and selective inhibitor of MET(IC50 : 1.7 nM).

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

Daclatasvir (EBP 883) (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

BMS-265246 is a potent and selective CDK1 2 inhibitor. Its chemical name is (4-[R-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-1H-indol-1-yl]-1H-pyrazolo[3,4-d] pyrimidine-6-amine), and it functions by targeting CDK1 and CDK2 to potentially disrupt cell cycle progression.

BMS-5 (LIMKi 3) is a highly potent LIMK inhibitor, exhibiting IC50 values of 7 nM for LIMK1 and 8 nM for LIMK2.

BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a novel anticancer agent targeting both topoisomerase (Topo) I and Topo II.

BMS-194449 is a full beta 3 agonist.

BMS-378806 (BMS-806) selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus.

Beclabuvir, also known as BMS-791325, is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. BMS-791325 inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 at 50% inhibitory concentrations (IC50) below 28 nM. In cell culture, BMS-791325 inhibited replication of HCV subgenomic replicons representing genotypes 1a and 1b at 50% effective concentrations (EC50s) of 3 nM and 6 nM, respectively, with similar (3 to 18 nM) values for genotypes 3a, 4a, and 5a. B

Linrodostat (BMS-986205) is a selective inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1).

Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium-labeled Apixaban. Apixaban is a reversible inhibitor of Factor Xa (Ki: 0.08 nM and 0.17 nM in human and rabbit).

BMS-2 is a Met/Flt-3/VEGFR2 tyrosine kinase inhibitor.

BMS-986143, an orally active, reversible BTK inhibitor with an IC50 value of 0.26 nM, is designed for autoimmune disease research. Additionally, it targets TEC, BLK, BMX, TXK, FGR, YES1, and ITK, exhibiting IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM, 19 nM, and 21 nM, respectively [1].

BMS-935177 is a reversible BTK inhibitor with IC50 value of 3 nM.

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

BMS-309403 sodium is a potent, orally active, selective inhibitor of adipocyte fatty acid binding protein (FABP4, aP2), with inhibitory constants (Ki) of <2 nM for FABP4, 250 nM for FABP3, and 350 nM for FABP5. It competitively binds to the fatty-acid-binding pocket of the protein, impeding the attachment of endogenous fatty acids. This compound enhances endothelial function in apolipoprotein E-deficient mice and cultured human endothelial cells, underlining its potential therapeutic benefits [1] [2] [3].

Letolizumab (BMS-986004), a monoclonal antibody directed at CD40L, is engineered to express a mutant IgG1 devoid of effector functions, such as Fc binding and complement fixation. It effectively reduces rejection and thromboembolism while extending survival time [1] [2] [3].

Brivanib (BMS-540215) is an ATP-competitive inhibitor targeting VEGFR2 with an IC50 of 25 nM, exhibiting moderate potency against VEGFR-1 and FGFR-1, and over 240-fold selectivity against PDGFR-β. Phase 3.

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the HCV NS5B RNA-dependent RNA polymerase, inhibiting recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 (IC50 < 28 nM).

Atazanavir-d6 is a deuterated compound of Atazanavir. Atazanavir has a CAS number of 198904-31-3. Atazanavir(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Pegdinetanib (BMS-844203; CT-322) is a selective inhibitor targeting VEGFR-2 (VEGFR), with dissociation constants (Kd) of 11 nM and 250 nM and half-maximal inhibitory concentrations (IC50) of 16 nM and 240 nM for human and murine VEGFR-2, respectively, and shows no affinity for VEGFR-1 or VEGFR-3, demonstrating antitumor activity [1].

BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202). BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase/Akt pathway, as evidenced by decreased Akt phosphorylation at Ser473. At doses that inhibited proliferation, the compound also caused a G0-G1 arrest and prevented nuclear accumulation of cyclin D1 in response to LR3 IGF-I. In Jurkat T-cell leukemia cells, this agent triggered apoptotic cell death via the mitochondrial pathway. BMS-554417 was orally bioavailable and significantly inhibited the growth of IGF1R-Sal tumor xenografts in vivo. BMS-554417 is a member of a novel class of IGF-IR/insulin receptor inhibitors that have potential......

BMS-378806 is a novel attachment inhibitor of HIV (EC50: 2.68±1.64nM, 26.5±3.5nM, 2.94±2.01nM,15.5±6.8nM, 3.46±0.81nM, 1.47±0.63nM and 0.85±0.13nM for LAI(T), SF-2(T),NL4-3(T), Bal(M), SF-162(M), JRFL(M) and TLAV(dual), respectively).

BMS-196085 is an effective and selective human β( 3) All agonists of adrenergic receptors, in β( 1) Partial agonist activity was 45%.

Relatlimab(BMS-986016) is a monoclonal antibody targeting human anti-LAG-3, generated by immunization of transgenic mice with human immunoglobulin carrying recombinant LAG-3 protein.Relatlimab has a blocking effect, blocking the interaction of LAG-3 MHC II (IC50: 0.67 nM) and LAG-3 FGL1 (IC50: 0.019 nM). Relatlimab is often used with Nivoluma to treat advanced melanoma.