Selective inhibitor of CDK1/cyclin B (IC50=4.2µM) with some P-glycoprotein-modulating properties (inhibitory activity ratio 1.26 at 7µM). Weakly inhibits CDK5/p25 (6% inhibition at 10µM) with no effect on CDK2/cyclin E and CDK4/cyclin D1 (IC50>100µM).
Product Details
Alternative Name: | 3-Acetyl-6-hydroxy-4-phenylbenzo[4,5]furo[2,3-b]pyridine, 1-Aza-9-oxafluorene 5b |
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Formula: | C19H13NO3 |
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MW: | 303.3 |
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Purity: | ≥95% (HPLC) |
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Appearance: | Off-white to brownish powder. |
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Solubility: | Soluble in DMSO. Insoluble in water or 100% ethanol. |
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Shipping: | Ambient Temperature |
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Long Term Storage: | +4°C |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes: B. Voigt, et al.; Bioorg. Med. Chem. Lett.
15, 823 (2005),
Abstract;
Evaluation of the first cytostatically active 1-aza-9-oxafluorenes as novel selective CDK1 inhibitors with P-glycoprotein modulating properties: K. Brachwitz, et al.; J. Med. Chem.
46, 876 (2003),
Abstract;
General Literature References
Probing novel 1-aza-9-oxafluorenes as selective GSK-3beta inhibitors: B. Voigt, et al.; ChemMedChem
3, 120 (2008),
Abstract;