|2-(5-氯-2-((3-(4-甲基哌嗪-1-基)丙基)氨基)嘧啶-4-基)-N-环丙基苯并[b]噻吩-4-酰胺|CsnPharm

CAS No.: 946518-61-2

Synonyms: Ly2409881

LY2409881 is a selective inhibitor of IKK2 with IC50 of 30 nM and IC50 for IKK1 and other common kinases is at least one log higher.

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

描述The NF-kB pathway plays a key role in multiple cellular processes, including immune signaling, inflammation, development, proliferation and survival. The activation of the upstream molecule, IKKα or β (IkB kinase), is required for NF-kB pathway and regulates NF-kB pathway via phosphorylation by specific IKK kinases and by autophosphorylation. LY2409881 is a selective IKK2 inhibitor with IC50 value of 30nM by in vitro kinase assay, with IC50s at least one log higher for IKK1 and other common kinases. Treatment with 10μM LY2409881 led to suppression of TNFα-induced phosphorylation of IκB in DLBCL cell line within 60 minutes. The block of constitute activation of NF-κB, shown as the exclusion of p50 from nuclear, can be observed in SUDHL2 cells exposure to 10μM LY2409881 for 4 hours. LY2409881 led to a concentration-dependent increase of apoptosis at concentration of 10 and 20μM in the DLBCL cell line SUDHL2 cells after 24 hours of exposure, inhibited survival and proliferation of the DLBLC cell line LY10 in both time (24-72h)- and dose-dependent manner and caused concentration-dependent apoptosis and cell death in MT2 cells after 48 hours of exposure at concentration ranging in 1-8μM. Intraperitoneal injections with LY2409881 twice weekly at dose of 50, 100, and 200 mg/kg all slowed the rate of tumor growth in SCID-beige mice implanted with LY10 cell-derived tumors.
动物研究
剂量
Mice: 50 mg/kg - 200 mg/kg^[1] (i.p.)

给药途径
i.p.)

动物研究
剂量	Mice: 50 mg/kg - 200 mg/kg^[1] (i.p.)
给药途径	i.p.)

实验方案

技术信息

CAS号	946518-61-2	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C24H29ClN6OS	运输	蓝冰
分子量	485.04	别名	Ly2409881

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