BMS-345541

Research use only, not for human use.

A potent and selective IKK-2 inhibitor with IC50 of 0.3 uM.

A potent and selective IKK-2 inhibitor with IC50 of 0.3 uM; less potent for IKK-1 (IC40=4 uM) and no activity against IKK-ε; inhibits LPS-stimulated TNFα, IL-1β, IL-8, and IL-6 in THP-1 cells with IC50 of1-5 uM; has excellent pharmacokinetics in mice.

BMS-345541 inhibits IKK-2 and IKK-1 in dose-dependent manner. BMS-345541 fails to inhibit a panel of both serine/threonine and tyrosine kinases at concentrations as high as 100 μM. MS-345541 at concentrations as high as 100 μM fails to block both the anisomycin-stimulated phosphorylation of c-Jun and LPS-stimulated activation of MAPKAP K2 in THP-1 cells, as well as the EGF-stimulated phosphorylation of STAT3 in H292 cells. BMS-345541 treatment results in a concentration-dependent inhibition of melanoma cell proliferation in SK-MEL-5, A375, and Hs 294T cells. BMS-345541 (0, 100 μM) shows apoptotic features as revealed by TUNEL staining and nuclear condensation.

BMS-345541 (10 mg/kg, p.o.) results in prolonged serum drug levels, with concentrations sustained at or above 1 μM for many hours in mice. BMS-345541 dose-dependently inhibits the production of TNFα measured in the serum of animals challenged with an intraperitoneal administration of LPS. BMS-345541 (0, 10, 25, and 75 mg/kg, p.o.) effectively inhibits SK-MEL-5 tumor growth in a dose-dependent manner in the mice. Tumor-bearing mice treated with 75 mg/kg of BMS-345541 show effective inhibition of growth of SK-MEL-5, A375, and Hs 294T tumors by 86±2.8%, 69±11% and 67±3.4%, respectively. BMS-345541 (30 and 100 mg/kg, p.o.) is effective in blocking both clinical and histological endpoints of inflammation and injury in mice.

BMS345541 hydrochloride | BMS-345541 hydrochloride | BMS 345541 hydrochloride

Immunology/Inflammation

IκB kinase (IKK)

IκB kinase (IKK)

Cancer

——

547757-23-3

291.7792

C14H18ClN5

>98% (HPLC)

10 mM in DMSO

CC1=CC2=C(C=C1)N=C(C3=NC=C(N23)C)NCCN.Cl

1,2-Ethanediamine, N1-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years