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ATM protein kinase inhibitor KU-55933, 10 mg  

ATM protein kinase inhibitor KU-55933, 10 mg

2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one

Synonyms: KU55933
selective and ATP specific inhibitor of ATM kinase, protein kinase inhibitor

More details

PKI-KU55933 -010

Availability: within 3 days

182,00 €

Background: KU-55933 is a potent and ATP specific inhibitor of Ataxia-Telangiectasia Mutated Kinase ATM (IC50 of 12.9 nmol/L and a Ki of 2.2 nmol/L). This potency is essentially restricted to ATM as it is at least 100-fold more potent than against the other PIKK family members (IC50 of ATR is > 100 µmol/L) and shows no activity against a panel of 60 unrelated kinases. Exposure of cells to KU-55933 resulted in a significant sensitization to the cytotoxic effects of ionizing radiation and to the DNA double-strand break-inducing chemotherapeutic agents. Since ATM is able to mediate full activation of Akt/PKB in response to insulin it was demonstrated that upon treatment of cancer cells with KU-55933 the phosphorylation of Akt induced by insulin and insulin-like growth factor is blocked. Furthermore, KU-55933 completely abrogates rapamycin-induced feedback activation of Akt.

Chemical Formula: C21H17NO3S2
Molecular Weight:  395.49 g/mol
Purity:  >99 %
Solubility:  soluble in DMSO
CAS number: 587871-26-9
Appearance: Pale-yellow solid
Manufacturer: Axon Medchem BV

Product specific literature references:

Hickson I, Zhao Y, Richardson CJ, Green SJ, Martin NM, Orr AI, Reaper PM, Jackson SP, Curtin NJ, Smith GC. (2004) “Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM.”Cancer     Res. 15;64(24):9152-9.

Lau A, Swinbank KM, Ahmed PS, Taylor DL, Jackson SP, Smith GC, O\'Connor MJ. (2005) “Suppression of HIV-1 infection by a small molecule inhibitor of the ATM kinase.” Nat Cell Biol. 7(5):493-500.

Li Y, Yang DQ.(2010)  “The ATM inhibitor KU-55933 suppresses cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt.” Mol CancerTher. 9(1):113-25.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.