<Suppliers Price>

CRT 0066854 hydrochloride

Names

[ CAS No. ]:
2250019-91-9

[ Name ]:
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]:

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H26ClN5S

[ Molecular Weight ]:
452.01

Related Compounds