KU-55933 | CAS:587871-26-9

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Name:KU-55933; 
Cat. No. :CS-0146
CAS No. :587871-26-9
Formula:C21H17NO3S2
M. Wt. : 395.49
Solubility:DMSO: 80 mg/mL (Need ultrasonic)

KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.IC50 & Target: IC50: 12.9 nM (ATM)[1]In Vitro: KU-55933 (10 μM) blocks the ionizing radiation-induced p53 serine 15 phosphorylation. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with an estimated IC50 of 300 nM. KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 specifically inhibits ATM but not the other DNA damage-activated PIKKs, ATR, and DNA-PK[1]. KU-55933 induces pATM, p53, E2F1 and pATR, noticeably upregulates the nuclear fraction of E2F1 at the 0.5 h time point[2]. Metformin increases ATM and AMPK phosphorylation, as well as SHP protein level in primary hepatocytes, and this stimulatory effect of metformin is repressed by a specific ATM kinase inhibitor KU-55933[3].

Kim YD, et al. Orphan nuclear receptor SHP negatively regulates growth hormone-mediated induction of hepatic gluconeogenesis through inhibition of STAT5 transactivation.J Biol Chem. 2012 Sep 12. Hickson I, et al. Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM. Cancer Res. 2004 Dec 15;64(24):9152-9 Khalil HS, et al. Pharmacological inhibition of ATM by KU55933 stimulates ATM transcription.Exp Biol Med (Maywood). 2012 Jun;237(6):622-34. Epub 2012 Jun 22.