KU-55933 Inhibitor CAS No. 587871-26-9

Cat. No.	Name	Size	Price
KI0139	KU-55933	5 mg	$112
	KU-55933	10 mg	$210
	KU-55933	50 mg	$650

Chemical Characteristic

Product Name	KU-55933
CAS No.	587871-26-9
Molecular Weight	395.49
Formula	C₂₁H₁₇NO₃S₂
Chemical Name	2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one
Smiles	c1(cc(=O)cc(o1)c1cccc2Sc3ccccc3Sc12)N1CCOCC1
Chemical Structure

Biological activities

KU-55933 is a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase (ATM). The IC50 of KU-55933 is 12.9 nM for ATM while the K_{i of KU-55933 binding to ATM is 2.2 nM. KU-55933 shows specificity with respect to inhibition of other phosphatidylinositol 3??kinase-like kinases. KU-55933 inhibits DNA-PK and PI3K and mTOR with IC50 of 2.5, 16.6 and 9.3 µM, respectively. Exposure of cells to KU-55933 results in a significant sensitization to the cytotoxic effects of ionizing radiation and to the DNA double-strand break-inducing chemotherapeutic agents, etoposide, doxorubicin, and camptothecin. Inhibition of ATM by KU-55933 also causes a loss of ionizing radiation-induced cell cycle arrest.^[1] In parental U251 and U87 glioma lines, the addition of KU-55933 to TMZ significantly increases cell killing compared to TMZ alone. In parental U251 and U87 glioma lines, the addition of KU-55933 to TMZ significantly increases cell killing compared to TMZ alone. ^[2] KU-55933 blocks the phosphorylation of Akt induced by insulin and insulin-like growth factor I in cancer cells that exhibit abnormal Akt activity. KU-55933 inhibits cancer cell proliferation by inducing G1 cell cycle arrest. KU-55933 treatment during serum starvation triggers apoptosis.^[3] KU-55933 not only suppresses p53 and nuclear factor-κB (NF-κB) activation but also notably increases radiation-induced DR5 surface expression. Moreover, KU-55933 down-regulates cFLIP (caspase-8 inhibitor) levels, and substantially enhances exogenous TRAIL-induced apoptosis.^[4]}

References

[1] Hickson I, 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. [2] Nadkarni A, et al. ATM inhibitor KU-55933 increases the TMZ responsiveness of only inherently TMZ sensitive GBM cells. J Neurooncol. 2012. [3] Li Y, 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. [4] Ivanov VN, et al. Inhibition of ataxia telangiectasia mutated kinase activity enhances TRAIL-mediated apoptosis in human melanoma cells. Cancer Res. 2009, 69(8), 3510-3519.

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