IKK Inhibitor III, BMS-345541 – CAS 445430-58-0 – Calbiochem

Descrição detalhada : A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50 ~4.0 µM) and does not inhibit IKKepsilon and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IkappaBalpha phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model., A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µM) and no activity towards IKKepsilon and a panel of more than 15 unrelated protein kinases even at concentrations as high as 100 µM. Inhibits cellular IkappaBalpha phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and joint destruction in a murine arthritis model.
Sinónimos : IKK Inhibitor III, BMS-345541 - CAS 445430-58-0 - Calbiochem; 4-(2?-Aminoethyl)amino-1,8-dimethylimidazo[1,2-a]quinoxaline
Fórmula molecula r: C14H17N5 · 2C2HF3O2
Armazenamento : 2-8C; 2-8C; 2-8C; 2-8C
Embalagem : 1X1MG