| Bioactivity | CRT0066854 is a potent and selective atypical PKC isoenzymes 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]. | ||||||||||||
| Invitro | CRT0066854 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 (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]. | ||||||||||||
| Name | CRT0066854 | ||||||||||||
| CAS | 1438881-19-6 | ||||||||||||
| Formula | C24H25N5S | ||||||||||||
| Molar Mass | 415.55 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
CRT0066854
CAS: 1438881-19-6 F: C24H25N5S W: 415.55
CRT0066854 is a potent and selective atypical PKC isoenzymes inhibitor. CRT0066854 is against full-length (FL) PKCι, PK
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