CRT 0066854 hydrochloride

Modify Date: 2024-01-15 16:44:26

CRT 0066854 hydrochloride Structure
CRT 0066854 hydrochloride structure
Common Name CRT 0066854 hydrochloride
CAS Number 2250019-91-9 Molecular Weight 452.01
Density N/A Boiling Point N/A
Molecular Formula C24H26ClN5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CRT 0066854 hydrochloride


CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively[1].

 Names

Name CRT0066854 hydrochloride

 CRT 0066854 hydrochloride Biological Activity

Description CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively[1].
Related Catalog
Target

PKCζ:639 nM (IC50)

ROCKII:620 nM (IC50)

In Vitro CRT0066854 hydrochloride displaces a crucial Asn-Phe-Asp motif that is part of the adenosine-binding pocket and engages an acidic patch used by arginine-rich PKC substrates[1]. CRT0066854 hydrochloride (0.2-1.2 μM; 6 days) is able to restore polarized morphogenesis in the dysplastic H-Ras spheroids, and the maximal proportion of spheroids with PSALs is at the lower dose of 1.2 μM[1].
References

[1]. Kjær S, 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. 2013 Apr 15;451(2):329-42.

 Chemical & Physical Properties

Molecular Formula C24H26ClN5S
Molecular Weight 452.01
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