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
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)
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