Analog of kenpaullone (Prod. No. BML-EI310) acting as a potent and ATP-competitive inhibitor of GSK-3β (IC50=18nM). Displays ~100-200 fold greater selectivity on GSK-3β than over CDK1/cyclin B and CDK5/p25 (IC50=2.0µM and 4.2µM, respectively).
Product Details
| Alternative Name: | 9-Bromo-7,12-dihydropyrido[3',2':2,3]azepino[4,5-b]indol-6(5H)-one, 1-AKP |
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| Formula: | C15H10BrN3O |
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| MW: | 328.2 |
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| CAS: | 676596-65-9 |
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| Purity: | ≥95% (HPLC, TLC) |
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| Appearance: | Off-white to brown powder. |
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| Solubility: | Soluble in DMSO; insoluble in water. |
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| Shipping: | Ambient |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stock solutions are stable for up to 6 months when stored at -20°C. |
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| Handling: | Protect from moisture. Protect from light. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
A chemical biology approach reveals period shortening of the mammalian circadian clock by specific inhibition of GSK-3beta: T. Hirota, et al.; PNAS USA
105, 20746 (2008),
Abstract;
Full Text
Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes: B. Voigt, et al.; Bioorg. Med. Chem. Lett.
15, 823 (2005),
Abstract;
1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta: C. Kunick, et al.; Bioorg. Med. Chem. Lett.
14, 413 (2004),
Abstract;
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