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PHA-767491
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C12H11N3O
- MW: 213.24
Description
PHA-767491 is an ATP-competitive dual inhibitor of the cell-cycle and transcriptional kinases CDC7 and CDK9, with IC50 values of 10 nM and 34 nM, respectively. PHA-767491 blocks DNA replication and pro-survival transcription, causing replication stress and cell death in cancer models. It shows preclinical antitumor activity and helps study T-cell function.
Key Features
- Dual CDC7 and CDK9 kinase inhibitor
- IC50: 10 nM for CDC7 and 34 nM for CDK9
- Blocks replication-origin firing and transcriptional elongation
- Induces replication stress and apoptotic cell death
Applications
- CDC7 and CDK9 kinase research
- DNA replication initiation and S-phase control
- RNA polymerase II transcriptional regulation
- MCL-1 and apoptosis studies
- Cancer-cell and T-cell activation models
More Information
| Parent CAS No. | 845714-00-3 |
|---|---|
| Chemical Name | 2-(Pyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one |
| SMILES | N1C=CC(C2=CC3C(=O)NCCC=3N2)=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C12H11N3O/c16-12-9-7-11(8-1-4-13-5-2-8)15-10(9)3-6-14-12/h1-2,4-5,7,15H,3,6H2,(H,14,16) |
| InChiKey | DKXHSOUZPMHNIZ-UHFFFAOYSA-N |
| CID | 11715767 |
| Short Description | CDC7/CDK9 inhibitor |
References
- DR Anderson et al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54.
- E Vanotti et al. Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships. J Med Chem. 2008 Feb 14;51(3):487-501.
- A Montagnoli et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65.
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