Aloisine A-CAS 496864-16-5-Calbiochem

半岛bd体育手机客户端 说明

一般描述

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 ?M for GSK-3α, GSK-3β, respectively), and c-Jun N-terminal kinase (JNK; IC₅₀= ~ 3 - 10 ?M). It inhibits several other enzymes (CK1, CK2, MAPKK, PKA, PKG, PKCs, and c-raf) poorly (IC₅₀≥ 100 ?M). Shown to arrest cells in both G₁and G₂phases (IC₅₀= 7 ?M and 10.5 ?M 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 ?M Forskolin (Cat. No. 344270) with high affinity (EC₅₀= 150 nM, 140 nM and 111 nM, respectively).
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 for Cdk1/cyclin B, 120 nM for Cdk2/cyclin A, 400 nM for Cdk2/cyclin E, and 160 nM for Cdk5/p25), glycogen synthase kinase-3 (GSK-3; IC₅₀= 500 nM for GSK-3α and 1.5 ?M for GSK-3β), and c-Jun N-terminal kinase (JNK; IC₅₀~3-10 ?M). Also inhibits extracellular signal-regulated kinases (ERKs; IC₅₀= 18 ?M for ERK1 and 22 ?M for ERK2), PIM1 (IC₅₀>10 ?M), and insulin receptor tyrosine kinase (IC₅₀= 60 ?M) at higher concentrations. Does not significantly inhibit Cdk4/cyclin D1, CK1, CK2, MAPKK, PKA, PKG, PKCs, or c-raf (IC₅₀= ≥ 100 ?M). Shown to arrest undifferentiated human teratocarcinoma cells (NT2) and differentiated post-mitotic neurons (hNT) in both G₁and G₂phases (IC₅₀= 7 ?M and 10.5 ?M, respectively). Also shown to selectively stimulate CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 ?M of Forskolin (Cat. No. 344270) with high affinity (EC 50= 150 nM, 140 nM and 111 nM, respectively).

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

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 ?M Forskolin, respectively
Primary Target
Cyclin-dependent kinases
Reversible: yes
Cell permeable: yes
Target 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 ?M for GSK-3α, GSK-3β, respectively
Product competes with ATP.

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Noel, S., et al. 2006.J. Pharm. Exp. Ther.,319,349.
Mettey, Y., et al. 2003.J. Med. Chem.46,222.

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	C16H17N3O
分子量	267.33

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	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 1
闪点(F)	Not applicable
闪点(C)	Not applicable