2250019-91-9

2250019-91-9 structure

Name: CRT 0066854 hydrochloride
Chemical Name: CRT0066854 hydrochloride
CAS Number: 2250019-91-9
Molecular Formula: C₂₄H₂₆ClN₅S
Molecular Weight: 452.01
Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
Create Date: 2020-06-01 09:18:10
Modify Date: 2024-01-15 16:44:26
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].

Name	CRT0066854 hydrochloride

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	Signaling Pathways >> Epigenetics >> PKC Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Research Areas >> Neurological Disease Signaling Pathways >> TGF-beta/Smad >> PKC Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK
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.

Molecular Formula	C₂₄H₂₆ClN₅S
Molecular Weight	452.01