Cdc7/Cdk9 Inhibitor CAS: 845714-00-3
MF: C12H11N3O
MW: 213.24
A potent, reversible, and ATP-competitive inhibitor of Cdc7 and Cdk9.

Cdc7/Cdk9 Inhibitor (CAS 845714-00-3)

Cdc7/Cdk9 Inhibitor | CAS 845714-00-3 is rated 5.0 out of 5 by 1.
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Synonym: PHA 767491; 2-Pyridin-4-yl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one
Application: 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
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cdc7/Cdk9 Inhibitor is 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 with Cdc7/Cdk9 Inhibitor results in a prevention of the activation of DNA replication origins without the inhibition of replication fork progression. Cdc7/Cdk9 Inhibitor is also reported to inhibit the proliferation of 61 cell lines in vitro (IC50 ≤ 10μM) and exhibit antitumor activity. Cdc7/Cdk9 Inhibitor is an inhibitor of MAPKAPK-2.


References

1. Montagnoli, A., et al. 2008. Nat Chem Biol. 4: 357-365. PMID: 18469809
2. Vanotti, E., et al. 2008. J. Med. Chem. 51: 487-501. PMID: 18201066
3. Anderson, D.R., et al. 2007. J. Med. Chem. 50, 2647-2654. PMID: 17480064

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), DMF (~0.3 mg/ml), and water (>25 mg/ml).
Storage :
Store at -20° C
Melting Point :
188.05° C (Predicted)
Boiling Point :
620.59° C at 760 mmHg (Predicted)
Density :
1.29 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
Cdc7 : IC50 = 10 nM; Cdk9: IC50 = 34 nM; GSK-3β: IC50 = 0.22 µM; Cdk2: IC50 = 0.24 µM; Cdk1: IC50 = 0.25 µM; Cdk5: IC50 = 0.46 µM; MK-2: IC50 = 0.47 µM; Plk1: IC50 = 0.98 µM; Chk2: IC50 = 1.1 µM
pK Values :
pKb: 5.69
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11715767
MDL Number :
MFCD11519962
SMILES :
C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3

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Certificate of Analysis

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Cdc7/Cdk9 Inhibitor  Product Citations

See how others have used Cdc7/Cdk9 Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 25843623  Chen, YH. et al. 2015. Mol. Cell. 58: 323-338.

Citations 1 to 1 of 1 total
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Rated 5 out of 5 by from An increase in PARP An increase in PARP-1 expression was observed in Jurkat cells by WB when comparing untreated cells with those that have been treated with Cdc7/Cdk9 inhibitor. -SCBT QC
Date published: 2015-03-31
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