A PKCι and PKCζ inhibitor (IC50s = 132 and 639 nM

CRT0066854 – 1 mg

Brand:
Cayman
CAS:
1438881-19-6
Storage:
-20
UN-No:
Non-Hazardous - /

CRT0066854 is an inhibitor of PKCι and PKCζ (IC50s = 132 and 639 nM, respectively).{46388} 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.  

 

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SKU: 28463 - 1 mg Category:

Description

A PKCι and PKCζ inhibitor (IC50s = 132 and 639 nM, respectively); an inhibitor of ROCK-II (IC50 = 620 nM); is selective for PKCι, PKCζ, and ROCK-II over typical PKCs and 98 other kinases in a panel at 1 µM; decreases viability of A549 lung carcinoma cells (IC50 = 3.47 µM); decreases colony formation in HeLa cells by 65% at 1 µM; impairs lumen formation in MDCK cells in a Matrigel™ assay and migration of NRK-49F cells in a wound assay

Formal name: (2S)-3-phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine

Synonyms: 

Molecular weight: 415.6

CAS: 1438881-19-6

Purity: ≥98%

Formulation: A crystalline solid

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