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CRT0066854
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C24H25N5S
- MW: 415.55
Description
Selective ATP-competitive inhibitor of the atypical PKC isoenzymes (IC50 values 639 nM and 132 nM, for full-length PKCζ, PKCι, respectively). CRT0066854 decreased colony formation in HeLa cells, inhibits LLGL2 phosphorylation and polarized epithelial morphogenesis, and impedes directed migration of NRK cells. A chemical tool to further dissect PKCζ and PKCι roles in establishing cell polarity and growth-factor-stimulated signalling pathways.
More Information
| Parent CAS No. | 1438881-19-6 |
|---|---|
| Chemical Name | (2S)-3-phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine |
| SMILES | C(NC1N=C(C2C=CN=CC=2)N=C2SC3CCCCC=3C2=1)[C@@H](N)CC1=CC=CC=C1 |&1:21,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H25N5S/c25-18(14-16-6-2-1-3-7-16)15-27-23-21-19-8-4-5-9-20(19)30-24(21)29-22(28-23)17-10-12-26-13-11-17/h1-3,6-7,10-13,18H,4-5,8-9,14-15,25H2,(H,27,28,29)/t18-/m0/s1 |
| InChiKey | NRHASZRDWOUMFD-SFHVURJKSA-N |
| CID | 70702288 |
| Short Description | PKC inhibitor |
References
- S Kjær 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.
- M Linch et al. Regulation of polarized morphogenesis by protein kinase C iota in oncogenic epithelial spheroids. Carcinogenesis. 2014 Feb;35(2):396-406.
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