Cdc7/Cdk9 Inhibitor: sc-311303. Western blot analysis of PARP-1 expression in untreated (A) and Cdc7/Cdk9 Inhibitor treated (B) Jurkat whole cell lysates. Antibody tested: PARP-1 (B-10): sc-74470.
Cdc7/Cdk9 Inhibitor (CAS 845714-00-3)
See product citations (1)
Alternate Names:
PHA 767491; 2-Pyridin-4-yl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one
Application:
Cdc7/Cdk9 Inhibitor is a potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9
CAS Number:
845714-00-3
Purity:
≥98%
Molecular Weight:
213.24
Molecular Formula:
C12H11N3O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
A cell-permeable pyrrolopyridinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9 (IC50 = 10 and 34 nM, respectively) Reported to have good selectivity over a panel of 31 other kinases, including GSK-3β, Cdk2, Cdk1, Cdk5, MK-2, Plk1, and Chk2 (IC50 = 0.22, 0.24, 0.25, 0.46, 0.47, 0.98, and 1.1 µM, respectively). It has been shown that cellular treatment of PHA76749 results in a prevention of the activation of DNA replication origins without the inhibition of replication fork progression. Also reported to inhibit the proliferation of 61 cell lines in vitro (IC50 ≤ 10 µM) and exhibit antitumor activity in both mice and rats in vivo.
Cdc7/Cdk9 Inhibitor (CAS 845714-00-3) References
- Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). | Anderson, DR., et al. 2007. J Med Chem. 50: 2647-54. PMID: 17480064
- Cdc7 kinase inhibitors: pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships. | Vanotti, E., et al. 2008. J Med Chem. 51: 487-501. PMID: 18201066
- A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. | Montagnoli, A., et al. 2008. Nat Chem Biol. 4: 357-65. PMID: 18469809
- Mechanisms of action of a dual Cdc7/Cdk9 kinase inhibitor against quiescent and proliferating CLL cells. | Natoni, A., et al. 2011. Mol Cancer Ther. 10: 1624-34. PMID: 21768328
- Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. | Li, W., et al. 2015. Curr Cancer Drug Targets. 15: 196-204. PMID: 25643258
- Repurposing of the CDK inhibitor PHA-767491 as a NRF2 inhibitor drug candidate for cancer therapy via redox modulation. | Liu, HY., et al. 2018. Invest New Drugs. 36: 590-600. PMID: 29297149
- Repression of Mcl-1 expression by the CDC7/CDK9 inhibitor PHA-767491 overcomes bone marrow stroma-mediated drug resistance in AML. | O' Reilly, E., et al. 2018. Sci Rep. 8: 15752. PMID: 30361682
- A Dual Inhibitor of Cdc7/Cdk9 Potently Suppresses T Cell Activation. | Chen, EW., et al. 2019. Front Immunol. 10: 1718. PMID: 31402912
- Targeting Inflammation, PHA-767491 Shows a Broad Spectrum in Protein Aggregation Diseases. | Chung, YH., et al. 2020. J Mol Neurosci. 70: 1140-1152. PMID: 32170713
- Increasing Brain Permeability of PHA-767491, a Cell Division Cycle 7 Kinase Inhibitor, with Biodegradable Polymeric Nanoparticles. | Rojas-Prats, E., et al. 2021. Pharmaceutics. 13: PMID: 33525757
- Dbf4-Cdc7 (DDK) Inhibitor PHA-767491 Displays Potent Anti-Proliferative Effects via Crosstalk with the CDK2-RB-E2F Pathway. | Pauzaite, T., et al. 2022. Biomedicines. 10: PMID: 36009559
Inhibitor of:
Cdc10, Cdc7, Cdk1/Cdk2, Cdk9, Integrin αM, Kin28, MAPKAPK-2, and Sox-8.Activator of:
GMF-β, and SKIV2L.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Cdc7/Cdk9 Inhibitor, 5 mg | sc-311303 | 5 mg | $270.00 |