bms-345541

Description: BMS-345541 (BMS345541; BMS 345541) is a novel, highly potent and selective IKK-1/2 inhibitor with potential anticancer and anti-inflammatory activity. It inhibits the catalytic subunits of IKK-2/1 with IC50s of 0.3 uM and 4 uM in cell-free assays, respectively. It demonstrate significant in vivo antitumor efficacy in human melanoma xenografts SK-MEL-5. In 4 human glioma cell lines, BMS-345541 treatment significantly blocked cell proliferation (80%-95%) at the concentration of 10 uM or higher and also inhibited IL-8 expression in a dose dependent manner (IC50> 2 uM). And similar result of BMS-34551 inhibition on IKK which induced cell apoptosis was verified in human melanoma cell lines SK-MEL-5, Hs 294T, and A375.

References: J Biol Chem. 2003; 278(3):1450-6; Inflamm Res. 2003; 52(12):508-11; Arthritis Rheum. 2003; 48(9):2652-9.

Related CAS #: 2320261-79-6 (TFA); 547757-23-3 (HCl); 445430-58-0 (free base); 445430-59-1 (2HCl);

Chemical Name: 1, 2-Ethanediamine, N-(1, 8-dimethylimidazo(1, 2-a)quinoxalin-4-yl)-

InChi Key: PSPFQEBFYXJZEV-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H17N5/c1-9-3-4-11-12(7-9)19-10(2)8-17-14(19)13(18-11)16-6-5-15/h3-4, 7-8H, 5-6, 15H2, 1-2H3, (H, 16, 18)

SMILES Code: NCCNC1=NC2=C(N3C1=NC=C3C)C=C(C)C=C2