Network Version
Product Name: | KU-55933 | |
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CAS No.: | 587871-26-9 | |
Cat. No.: | HY-12016 | |
MWt: | 395.49 | |
Formula: | C21H17NO3S2 | |
Purity : | >98% | |
Solubility: | DMSO : 80 mg/mL (202.28 mM; Need ultrasonic) | |
Mechanisms: | Target: Cancer | |
Biological Activity: | ||
KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is 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]. |
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