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Basic Information
English Name 2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one  
Synonym ATM Kinase Inhibitor  
CAS 587871-26-9  
Molecular Formula C21H17NO3S2  
Molecular Weight 395.49  

Physical And Chemical Properties bp

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Dangerous Description  
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KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 13 and 2.2 nM, respectively; highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.  

Other Infomation

KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 13 and 2.2 nM, respectively; highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
IC50 Value: 13 nM
Target: ATM
in vitro: KU-55933 inhibits DNA-PK and PI3K with IC50 of 2.5 μM and 16.6 μM, respectively. Besides, KU-55933 also prevents the activity of mTOR with IC50 of 9.3 μM. KU-55933 is active at the cellular level in ablating a well-characterized ATM-dependent phosphorylation event. KU-55933 has a dose-dependent effect in inhibiting this ATM-dependent phosphorylation event with IC50 of 300 nM. KU-58050 does not prevent the ATM-dependent phosphorylation of p53 serine 15 until a dose of 30 μM. Addition of KU-55933 has no appreciable effects on UV-induced phosphorylation of H2AX on serine 139, NBS1 on serine 343, CHK1 on serine 345, and SMC1 on serine 966. In stark contrast to the UV responses, KU-55933 ablates the ionizing radiation-induced phosphorylation of these ATM substrates. KU-55933 sensitizes HeLa cells to a range of ionizing radiation doses. KU-55933 inhibits the phosphorylation of Akt induced by growth factors in cancer cells. KU-55933 suppresses the proliferation of cancer cells. Furthermore, suppression of ATM by KU-55933 improves survival, probably via prevention of downstream activation of TAp63α.
in vivo: Suppression of ATM-dependent STAT3 activation by KU-55933 enhances TRAIL-mediated apoptosis through up-regulation of surface DR5 expression, whereas suppression of both STAT3 and NF-κB appeares to be involved in down-regulation of cFLIP accompanied by an additional increase in apoptotic levels. The ATM inhibitor KU-55933 affectes TRAIL-mediated apoptosis more strongly than the JAK2 inhibitor, AG490, or overexpression of STAT3β.

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