MedChemExpress LLC (MCE)

MedChemExpress - Model BMS-265246 - 582315-72-8

BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research[1][2][3].

BMS-265246

MCE China：BMS-265246

Brand：MedChemExpress (MCE)

Cat. No.HY-15275

CAS：582315-72-8

Purity：98.92%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research.

In Vitro：BMS-265246 binds at the ATP site and shows cytotoxic activity in ovarian cancer cell (A2780), with an IC50 of 0.76 μM[1]. BMS-265246 (0-10 μM) can dose dependently increase iTreg cell differentiation[2]. BMS-265246 (9 nM, 24 h) inhibits the ability of CHI3L1 to stimulate epithelial cells ACE2 and SPP[3]. BMS-265246 (1 μM, 1 h) prevents E2 induction of EGF3, AREG and CXCL12 in MCF7 cells[4]. BMS-265246 is able to cooperate with Tamoxifen to induce apoptosis in MCF7 cells[4].

IC50 & Target：CDK1/cycB 6 nM (IC50) CDK2/Cyc E 9 nM (IC50) CDK4/cycD 230 nM (IC50)

References：

[1]. Misra RN, Xiao H, Rawlins DB et al. 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8. [Content Brief]

[2]. Gu H, et al. Inhibition of CDK2 promotes inducible regulatory T-cell differentiation through TGFβ-Smad3 signaling pathway. Cell Immunol. 2014 Jul;290(1):138-44. [Content Brief]

[3]. Kamle S, et al. Chitinase 3-like-1 is a therapeutic target that mediates the effects of aging in COVID-19. JCI Insight. 2021 Nov 8;6(21):e148749. [Content Brief]

[4]. Scott GK, et al. ERpS294 is a biomarker of ligand or mutational ERα activation and a breast cancer target for CDK2 inhibition. Oncotarget. 2016 Oct 18;8(48):83432-83445. [Content Brief]

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