产品属性:
产品名称
规格
CAS号
型号
CRT0066854
1mg 5mg 10mg
1438881-19-6
EY-Y0165475
Cas No.1438881-19-6
别名 N/A
化学名 N/A
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 产品描述: 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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