公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! 抑制剂描述: 产品名称:BMS-345541 hydrochloride 产品别名:见爱必信官网 英文别名:BMS-345541 hydrochloride 靶点:IKK CAS:547757-23-3 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: 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。 溶解性:DMSO :29.18 mg/mL(mM) Water :29.18 mg/mL(mM) 体外研究: 体内研究: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. 产品信息订购:
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