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Merck
CN

217697-M

Cdk1 Inhibitor III

The Cdk1 Inhibitor III, also referenced under CAS 440362-74-3, controls the biological activity of Cdk1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Cdk1 Inhibitor III, Ethyl-(6-hydroxy-4-phenylbenzo[4,5]furo[2,3-b])pyridine-3-carboxylate

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About This Item

Empirical Formula (Hill Notation):
C20H15NO4
CAS Number:
Molecular Weight:
333.34
UNSPSC Code:
12352200
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assay

≥95% (HPLC)

form

powder

potency

28.8 μM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

brown

solubility

ethanol: 10 mg/mL, DMSO: 20 mg/mL

storage temp.

2-8°C

General description

This product has been discontinued.



A cell-permeable 1-aza-9-oxafluorene compound that acts as a highly selective Cdk1/cyclin B inhibitor (IC50 = 28.8 µM) with very little activity against Cdk5/p25, Cdk2/E, or Cdk4/D1. Unlike other Cdk inhibitors, it exhibits potent inhibitory effect against P-glycoprotein-mediated MDR (multidrug resistance) in cancer cells (~9-fold more potent than verapamil). Its special bifunctional cytostatic property makes it an excellent tool for research in cancer treatment.

A cell-permeable, highly selective Cdk1/cyclin B inhibitor (IC50 = 28.8 µM). Exhibits only low inhibitory activity against Cdk5/p25, Cdk2/cyclin E, and Cdk4/cyclin D1. Unlike other Cdk inhibitors has also been reported to have potent inhibitory effects on P-glycoprotein-mediated multidrug resistance (MDR) in cancer cells (~9-fold more potent than verapamil). Its unique bifunctional cytostatic properties make it an attractive tool in cancer research.

Biochem/physiol Actions

Primary Target
Cdk1/cyclin B

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Brachwitz, K., et al. 2003. J. Med. Chem.46, 876.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)


Regulatory Information

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