BMS-345541高度选择性抑制IKK-2和IKK-1的催化亚基，IC50分别为0.3 μM和4 μM。在THP-1单核细胞中，BMS-345541剂量依赖性地抑制TNF-α刺激的IκBα的磷酸化，IC 50为4 μM。BMS-345541抑制THP-1细胞中脂多糖刺激肿瘤坏死因子，白细胞介素-1β，白介素-8和白介素-6的， IC 50值 在1到 5 μM范围内。 BMS-345541以相互排斥的方式结合在多肽抑制剂上，该多肽抑制剂和IκBα 26-42 氨基酸 序列一致，除了丝氨酸-32和丝氨酸-32改变为天冬氨酸。

>98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

BMS-345541；N-(1,8-二甲基咪唑并[1,2-A]喹喔啉-4-基)-1,2-乙二胺盐酸盐

固体粉末

DMSO ：29.18 mg/mL（mM）

Water ：29.18 mg/mL（mM）

IKK

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.

Activity of the selective IκB kinase inhibitor BMS-345541 against T-cell acute lymphoblastic leukemia: involvement of FOXO3a.
Buontempo F,et al. Cell Cycle. 2012 Jul 1;11(13):2467-75. PMID:

分子结构图