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CRT0066854
- Optical Purity: Optically pure
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C24H25N5S
- MW: 415.55
Description
CRT0066854 is a selective, ATP-competitive inhibitor of atypical protein kinase C (aPKC) isoenzymes, targeting full-length PKCι (IC50 = 132 nM) and PKCζ (IC50 = 639 nM). It serves as a valuable pharmacological tool to investigate aPKC roles in cell polarity, anchorage-independent growth, and growth-factor signaling.
PKC pharmacology drives key discoveries in translational oncology and cellular disease pathology. CRT0066854 supports mechanistic studies of atypical PKC isoforms and broader AGC kinase signaling across biochemical, cellular, and disease-model assays.
Key Features
- Atypical PKC inhibitor
- IC50: 132 nM againist PKCι and 639 nM against PKCζ
- Binds the kinase ATP-pocket to block catalytic activity
- Blocks downstream LLGL2 phosphorylation to disrupt cell architecture
Applications
- PKC pharmacology and target-validation studies
- PKC pathway and signaling assays
- Oncology studies in translational model systems
- Cell Motility Modeling
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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