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经验配方 CAS号 C₁₆H₁₇N₃O 496864-16-5 描述 概述 A cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. Acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks; IC50 = 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively), glycogen synthase kinase-3 (GSK-3; IC50 = 500 nM and 1.5 µM for GSK-3α, GSK-3β, respectively), and c-Jun N-terminal kinase (JNK; IC50 = ~ 3 - 10 µM). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC50 ≥ 100 µM). Shown to arrest cells in both G1 and G2 phases (IC50 = 7 µM and 10.5 µM for undifferentiated human teratocarcinoma cells NT2 and differentiated postmitotic neurons hNT, respectively). Shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM Forskolin (Cat. No. 344270) with high affinity (EC50 = 150 nM, 140 nM and 111 nM, respectively). 产品目录编号 128125 品牌系列 Calbiochem®
同义词 RP107, 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine 参考 参考 Noel, S., et al. 2006. J. Pharm. Exp. Ther. , 319, 349.
Mettey, Y., et al. 2003. J. Med. Chem. 46, 222.产品信息 CAS号 496864-16-5 具有ATP竞争性 Y 形式 Yellow solid Hill配方 C₁₆H₁₇N₃O 化学配方 C₁₆H₁₇N₃O Molar Mass 267.3 可逆 Y 结构配方图像 生物信息 主靶 Cyclin-dependent kinases 主靶IC50 150 nM, 120 nM, 400 nM, and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively; 500 nM and 1.5 µM for GSK-3α, GSK-3β, respectively 主靶Ki EC50 = 150 nM, 140 nM and 111 nM, in stimulating CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 µM Forskolin, respectively 纯度 ≥95% by HPLC 理化信息 细胞可渗透 Y 溶解度 DMSO 储存和货运信息 货运代码 Ambient Temperature Only
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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