bms 2

BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative. BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively. BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy.

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

BMS 599626 2HCl (873837-23-1(HCl)) (AC480 dihydrochloride) is a selective inhibitor of HER1 and HER2 (IC50s: 20 nM and 30 nM), ~8-fold less potent to HER4, >100-fold to Lck, VEGFR2, c-Kit, MET, etc.

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.

BMS CCR2 22 is a potent and selective antagonist of CCR2 with calcium flux IC50 of 18 nM, chemotaxis IC50 of 1 nM, and binding IC50 of 5.1 nM.

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

BMS-309403 is an effective, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.

Deucravacitinib (BMS-986165) inhibits IL-12/23 and type I IFN pathways[1][2]. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases. Which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain.

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.

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

BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1/PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction.

BMS-823778 is a potent inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) for the study of type 2 diabetes.

Muraglitazar (BMS-298585) is a PPAR α/γ dual agonist for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα and PPARγ with EC50 of 320 nM and 110 nM respectively.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

BMS-345541 (IKK Inhibitor III) is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

BMS-265246 is a potent and selective CDK1/2 inhibitor.

BMS-986172 is an orally active, highly selective inhibitor of MGAT2, demonstrating inhibitory concentrations (IC50) of 4.6 nM for human MGAT2 (hMGAT2) and 20 nM for mouse MGAT2 (mMGAT2). It exhibits a half-life (T1/2) greater than 120 minutes in vitro and is known to decrease food intake and body weight. This compound is considered promising for the research of metabolic disorders, including obesity and non-alcoholic steatohepatitis (NASH) [1].

(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC 50 >1μM for mGluR5 receptor [1] . BMS-984923 is a potent mGluR5 silent allosteric modulator [2] .

Gosuranemab (BMS-986168), a humanized IgG4 anti-tau monoclonal antibody, specifically targets human N-terminal tau residues 15-22. It holds potential for Alzheimer’s disease (AD) research [1] [2].

BMS-183920 is a diacid, potent angiotensin II receptor antagonist that improves Caco-2 cell permeability and in vivo oral absorption. The relative degree of hydrolysis (biological activation) and prodrug metabolism determines whether substantial improveme

BMS-767778, a DPP-4 inhibitor, is used potentially for the treatment of type 2 diabetes.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2). It is in development for the treatment of type 2 diabetes mellitus (T2DM). It inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney.

Avagacestat (BMS-708163) (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

BMS-605541 is a potent and selective inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2) kinase activity(Ki=49 nM).

Brivanib Alaninate (BMS-582664) is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression.

Saxagliptin (BMS-477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 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.

AAK1-IN-1 (example 123) is an AAK1 (adaptor associated kinase 1) inhibitor with an IC50 of 2.2 nM. AAK1-IN-1 can be used for neurodegenerative diseases research[1]. Adaptor associated kinase 1 (AAK1) is a member of the Arkl/Prkl family of serine/threonine kinases. AAKl mRNA exists in two splice forms termed short and long. The long form predominates and is highly expressed in brain and heart. AAKl is enriched in synaptosomal preparations and is co-localized with endocytic structures in cultured cells. AAKl modulates clatherin coated endocytosis, a process that is important in synaptic vesicle recycling and receptor-mediated endocytosis[1]. [1]. Guanglin Luo, et al. Biaryl kinase inhibitors. WO2015153720A1.

Beludavimab (BMS 4182137; VIR 7832), a monoclonal antibody, specifically targets the spike glycoprotein of SARS-CoV-2. It effectively binds to the receptor-binding domain of the recombinant spike protein (S-RBD) with an equilibrium concentration (EC50) of 14.9 ng/mL and a dissociation constant (Kd) of 0.21 nM [1].

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].

Beclabuvir (BMS-791325) is a potent NS5A replication complex inhibitor that inhibits the activity of the NS5B protein expressed by HCV genotypes 1, 2, 4, and 5 and is used in the study of HCV infection.

BMS-645737 is an inhibitor of vascular endothelial growth factor (VEGF) receptor-2 and fibroblast growth factor (FGF) receptor-1. BMS-646737 has anti-angiogenic activity and was evaluated in nonclinical studies as a treatment for cancer.

Alvespimycin hydrochloride (BMS 826476) is a potent HSP90 inhibitor with IC50 of 62 nM. Phase 2.

BMS-986235 (LAR-1219) is a selective and orally active agonist of formyl peptide receptor 2 (FPR2) with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 can be used in studies about the prevention of heart failure.

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

BMS-347070 is a COX-2 inhibitor.

Pegdinetanib (BMS-844203; CT-322) is a selective inhibitor targeting VEGFR-2 (VEGFR), exhibiting 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. It demonstrates no affinity for VEGFR-1 or VEGFR-3. Its effectiveness extends to antitumor activity [1].

BMS-681 is an orthosteric antagonist of chemokine receptor 2 (CCR2) that forms a ternary complex with CCR2 and its allosteric antagonist, CCR2-RA-[R]. Together, the complex inhibits chemokine binding with BVMS-681 in the orthosteric pocket and CCR2-RA-[R] in the intracellular allosteric G-protein binding site. When chemokine binding is inhibited, modulation responses implicated in several inflammatory and neurodegenerative diseases, including atherosclerosis, multiple sclerosis, asthma, neuropathic pain, diabetic nephropathy, and cancer can be controlled. This action occurs as the migration of monocytes, immature dendritic cells, and T-cell subpopulations towards endogenous CC chemokine ligands is mediated.

Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM).

Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor.

BMS 753 is an agonist of isotype-selective retinoic acid receptor α (RARα, Ki= 2 nM).

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-345541 hydrochloride is a selective IKK inhibitor (IKK2 and IKK1 with IC50 of 0.3 μM and 4 μM,respectively).

Crexavibart (BMS-986413; C-144-LS), an IgG1 λ2 antibody, specifically targets the receptor-binding domain of the SARS-CoV-2 spike (S) glycoprotein [1].

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

BMS-279700 is a potent oral activity inhibitor that is part of a new family of aniline 5-azimidazolaquoxaline analogs and has excellent anti-inflammatory activity in vivo, as well as in vitro activity against p56LCK and T cell proliferation, blocking the

BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist. With IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects[1][2].

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.