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CRT0066854
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CRT0066854图片
CAS NO: 1438881-19-6
包装与价格：
包装 价格(元)
1mg 电议
5mg 电议
10mg 电议

半岛bd体育手机客户端 介绍
CRT0066854 是一种有效的选择性非典型 PKC 同工酶抑制剂。
Cas No. 1438881-19-6
Canonical SMILES N[C@@H](CC1=CC=CC=C1)CNC2=C3C(SC4=C3CCCC4)=NC(C5=CC=NC=C5)=N2
分子式 C24H25N5S
分子量 415.6
溶解度 DMSO: 30 mg/ml
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

CRT0066854 is an inhibitor of PKCΙ and PKCζ (IC50s = 132 and 639 nM, respectively).1 It also inhibits the Rho-associated kinase II (ROCK-II) kinase domain (IC50 = 620 nM). It is selective for these atypical PKCs and ROCK-II over typical PKCs and 98 other kinases in a panel at 1 μM. CRT0066854 decreases phosphorylation of the atypical PKC substrate lethal giant larvae 2 (LLGL2) in HEK293 cells expressing PKCΙ and LLGL2. It decreases viability of A549 lung carcinoma cells (IC50 = 3.47 μM) and decreases colony formation in HeLa cells by 65% when used at a concentration of 1 μM. CRT0066854 impairs lumen formation in MDCK cells in a Matrigel? assay and migration of NRK-49F cells in a wound assay.

References
1. Kj?r, S., Linch, M., Purkiss, A., et al. Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes. Biochem. J. 451(2), 329-342 (2013).
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