bms 1

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

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.

Delcasertib acetate is a selective δ protein kinase C (δPKC) inhibitor for the study of acute myocardial infarction and pain.

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).

Ixabepilone (Azaepothilone B) is an orally bioavailable microtubule inhibitor. It binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis.

BMY-14802 hydrochloride (BMS 181100 hydrochloride) is a selective antagonist of σ receptor (IC50 = 112 nM) with antipsychotic effects. BMY-14802 hydrochloride is an agonist of the α1-adrenergic receptor and 5-HT1A.

Peliglitazar is a activator of α/γ peroxisome proliferator-activated receptor.

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.

LIMK1 inhibitor BMS-4 is a compound targeting LIM Kinase (LIMK) 1 2, specifically inhibiting the phosphorylation of its substrate cofilin, while remaining noncytotoxic on A549 cells.

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

Saxagliptin hydrate (Onglyza hydrate) is a selective and reversible DPP4 inhibitor (IC50: 26 nM; Ki: 1.3 nM).

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker whose mechanism of action involves antagonizing the Angiotensin 2 Receptor.

Atazanavir sulfate (BMS-232632 sulfate) is an azapeptide and HIV-protease inhibitor used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antivirals to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has not been convincingly implicated in cases of clinically apparent liver injury with jaundice.

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-488043 is a novel and unique oral small molecule HIV fusion inhibitor that inhibits the attachment of Human Immunodeficiency Virus type 1 (HIV-1) to CD4(+) lymphocytes.BMS-488043 is used for the treatment of immune disorders, infections, and genitourinary disorders, and can be used in the study of HIV infect

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-1166-N-piperidine-CO-N-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1) programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1 PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1 PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1 PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.

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

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.

BMS-986020 (AM152) is a selective LPA1 antagonist.

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).

BMS-986242 is an orally active, potent, and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, suitable for cancer research.

BMS-1001 is a potent inhibitor of PD-1 PD-L1 interaction(IC50 : 2.25 nM, in a homogenous time-resolved fluorescence binding assay).

BMS-191011 (BMS-A) is an activator of large-conductance calcium-activated potassium (BKCa) channels ,effective in stroke models

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.

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1 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-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by PXR transactivation, poor water so

BMS-248360 is a potent, orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptors, respectively. BMS-248360 demonstrates hypertensive effects[1].

BMS-823778 hydrochloride is a potent, selective, and orally active inhibitor of 11β-HSD1 (11β-Hydroxysteroid Dehydrogenase Type 1), with an IC50 (half maximal inhibitory concentration) of 2.3 nM against the human enzyme.

(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923, exhibiting an EC50 >1μM for the mGluR5 receptor [1]. BMS-984923, in contrast, is a potent mGluR5 silent allosteric modulator [2].

BMS 310705 (21-Aminoepothilone B), an Epothilone B analog, specifically targets malignancies including ovarian, renal, bladder, and lung carcinoma. It significantly induces apoptosis through the mitochondrial-mediated pathway [1].

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

BMS-378806 is an orally bioavailable HIV-1 inhibitor that interferes with gp120-CD4 interaction.

Peginterferon lambda-1a (BMS-914143) is a monoclonal antibody targeting IFNLR1, composed of IFNL1 conjugated to pegol [1].

Beludavimab (BMS 4182137; VIR 7832), a monoclonal antibody, specifically targets the spike glycoprotein of SARS-CoV-2, effectively binding 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].

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-332 is a dual inhibitor of the lipid kinases DGKα and DGKζ, demonstrating half-maximal inhibitory concentrations (IC50) of 0.005 μM for DGKα and 0.001 μM for DGKζ [1].

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-663749 lysine is used as a phosphonooxymethyl prodrug 4 for HIV-1 attachment inhibitor.

BMS-986318 is a potent nonbile acid FXR agonist with EC50 values of 53 nM (FXR Gal4) and 350 nM (SRC-1 recruitment assays). It has a favorable ADME profile and demonstrates effectiveness in mouse models of liver cholestasis and fibrosis caused by bile duct ligation. BMS-986318 is used in research on nonalcoholic steatohepatitis.

Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).