Product Description
KU55933 is an ATP-competitive, thioanthrene-pyranone-based inhibitor of ATM kinase with an IC50 of 13 nM and Ki of 2.2 nM and >100-fold selectivity over PI3K related kinases. [1] KU55933 inhibits cell proliferation by inducing G1 cell cycle arrest by downregulation of cyclin D1 synthesis in MDA-MB-453 breast cancer cells and PC-3 prostate cancer cells. [2] KU55933 inhibits insulin- and IGF1-stimulated Akt phosphorylation at both Ser473 and Thr308. [2] ATM cellular inhibition by KU55933 was demonstrated in additional phosphorylation targets, including p53 Ser15, H2AX Ser139, NBS1 Ser343, Chk1 Ser345, and SMC1 Ser966. [1]KU55933 is being studied as a radiosensitizer, having been shown to sensitize HeLa cells to the effects of topoisomerase inhibitors, etoposide, doxorubicin, amsacrine, and camptothecin. [1] When in combination with rapamycin, KU55933 induces apoptosis and arrests any induced feedback activation of Akt. [2]
Technical information:
| Chemical Formula: | C21H17NO3S2 | |
| CAS #: | 587871-26-9 | |
| Molecular Weight: | 395.49 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | KU-55933, KU 55933, KU55933 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Hickson et al., Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer Res. 2004, 64(24), 9152-9159. Pubmed ID: 15604286 |
| 2. | Li et al., The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt. Mol. Cancer. Ther. 2010, 9(1), 113-125. Pubmed ID: 20053781 |
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