| 规格: | 98% |
| 分子量: | 415.6 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
Background:
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.
参考文献
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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