Cdk1/5 Inhibitor InhibitorA 3-amino substituted pyrazoloquinoxaline compound and selective inhibitor of Cdk1/Cdk5

Cdk1/5 Inhibitor Inhibitor (CAS 40254-90-8)

Cdk1/5 Inhibitor | CAS 40254-90-8 is rated 5.0 out of 5 by 1.
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Synonym: 3-Amino-1H-pyrazolo[3,4-b]quinoxaline
Application: A 3-amino substituted pyrazoloquinoxaline compound and selective inhibitor of Cdk1/Cdk5
CAS Number: 40254-90-8
Purity: ≥95%
Molecular Weight: 185.2
Molecular Formula: C9H7N5
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cdk1/5 Inhibitor is a 3-amino substituted pyrazoloquinoxaline compound that acts as a selective inhibitor of Cdk1 and Cdk5 (IC50 = 600 nM for Cdk1/cyclin B and 400 nM for Cdk5/p25. Cdk1/5 Inhibitor is also shown to inhibit GSK-3β with (IC50 > 10 μM). Cdk1/5 Inhibitor does not inhibit Cdc25 phosphatase activity (IC50 > 10 μM).


References

1. Ortega, Miguel A., et al., 2002. Pyrazolo[3,4-b]quinoxalines. A new class of cyclin-dependent kinases inhibitors. Bioorganic & medicinal chemistry. 10(7): 2177-84. PMID: 11983514

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml).
Storage :
Store at 4° C
Melting Point :
175.08° C (Predicted) (tautomer)
Boiling Point :
522.8° C at 760 mmHg (Predicted) (tautomer)
Density :
1.57 g/cm3 (Predicted) (tautomer)
Refractive Index :
n20D 1.9 (Predicted)
IC50 :
Cdk5/p35: IC50 = 0.4 µM; Cdk1/cyclin B: IC50 = 0.6 µM; GSK-3&beta: IC50 = 1 µM; Cdc25 phosphatase activity: IC50 = >10 µM
pK Values :
pKa: 7.4 (Predicted), pKb: 3.61 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
438981
MDL Number :
MFCD04038461
SMILES :
C1=CC2=NC3=C(NN=C3N=C2C=C1)N

Download SDS (MSDS)

Certificate of Analysis

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Cdk1/5 Inhibitor Inhibitor  Product Citations

See how others have used Cdk1/5 Inhibitor Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 27378523  Chen, Z. et al. 2016. Sci Rep. 6: 29090.

PMID: # 25013173  Bounedjah, O. et al. 2014. Nucleic Acids Res. 42: 8678-91.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Ortega Ortega, MA. et al. (PubMed 11983514) were the first to identify pyrazolo[3,4-b]quinoxalines as sub-micromolar inhibitors of Cdk1/5. -SCBT Publication Review
Date published: 2015-05-14
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