半岛bd体育手机客户端 说明
一般描述
A cell-permeable ureidocarboxamido thiophene compound that acts as a potent, reversible, and ATP-competitive inhibitor of IKK-2 (IC50= 18 nM) with selectivity over IKK-1, JNK and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50in the range of 0.15-2.5 ?M) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50= 100 nM). Further reduces paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg). A 10 mM (500 ?g/179 ?l) solution of IKK-2 Inhibitor IV (Cat. No. 401484) in DMSO is available.
A cell-permeable, reversible, ATP-competitive, and potent inhibitor of IKK-2 (IC50= 18 nM) that exhibits selectivity over IKK-1, JNK, and p38 MAPK. Inhibits TNF-α production in human monocytes (IC50in the range of 0.15-2.5 ?M) and blocks IL-8 and IL-6 production by synovial fibroblasts (IC50= 100 nM). Shown to reduce paw oedema in rat arthritis model (~100% inhibition at a dose of 30 mg per kg).
包装
500 μg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target IC50: 18 nM against IKK-2
Primary Target
IKK-2
Product competes with ATP.
Reversible: yes
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Podolin, P.L., et al. 2005.J. Pharmacol. Exp. Ther.312,373.
Karin, M., et al. 2004.Nat. Rev. Drug Discov.3,17.
Roshak, A.K., et al. 2002.Inflamm. Res.51,S4.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C12H10FN3O2S |
分子量 | 279.29 |
MDL编号 | MFCD09037541 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem? |
储存条件 | OK to freeze protect from light |
颜色 | pale yellow |
溶解性 | DMSO: 10 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
Sigma-Aldrich