Selective inhibitor of CDK1 (IC50=28.8µM) with P-glycoprotein-modulating properties (inhibitory activity ratio 9.5 at 7µM). Weakly inhibits CDK5 (6% inhibition at 10µM) with no effect on CDK2 and CDK4 (IC50>100µM).
Product Specification
| Alternative Name: | Ethyl-(6-hydroxy-4-phenylbenzo[4,5]furo[2,3-b])pyridine-3-carboxylate, 1-Aza-9-oxafluorene 5a |
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| Formula: | C20H15NO4 |
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| MW: | 333.3 |
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| Purity: | ≥95% (HPLC) |
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| Appearance: | Brownish powder. |
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| Solubility: | Soluble in DMSO or 100% ethanol. Insoluble in water. |
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| Shipping: | Ambient |
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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
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.; Chem. Med. Chem.
3, 120 (2008),
Abstract;
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes: B. Voigt, et al.; Bioorg. Med. Chem. Lee.
15, 823 (2005),
Abstract;
