性能参数

产品名称

CRT0066854

规格

1mg 5mg 10mg

货号

GOY-Y2204

 含量

>98.00%

CAS

1438881-19-6

别名

N/A

化学名

N/A

分子式

C24H25N5S

分子量

分子 415.6

溶解度

DMSO: 30 mg/ml

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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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