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Products are for research use only. Not for human use. We do not sell to patients.
(KU 55933; KU55933)
KU-55933 Chemical Structure
|Product name: KU-55933|
|Cat. No.: HY-12016|
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
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.
|M.Wt||395.49||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥48mg/mL Water <1.2mg/mL Ethanol ≥11mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.5285 mL||12.6425 mL||25.2851 mL|
|5 mM||0.5057 mL||2.5285 mL||5.0570 mL|
|10 mM||0.2529 mL||1.2643 mL||2.5285 mL|
. Choi S, Srivas R, Fu K, Hood BL, Dost B, Gibson GA, Watkins SC, Van Houten B, Bandeira N, Conrads T, Ideker T, Bakkenist CJ.Quantitative proteomics reveals ATM kinase-dependent exchange in DNA damage response complexes.J Proteome Res. 2012 Aug 21.
. Kim YD, Li T, Ahn SW, Kim DK, Lee JM, Hwang SL, Kim YH, Lee CH, Lee IK, Chiang JY, Choi HS.Orphan nuclear receptor SHP negatively regulates growth hormone-mediated induction of hepatic gluconeogenesis through inhibition of STAT5 transactivation.J Biol Chem. 2012 Sep 12.
CGK 733 is a small molecule inhibitor reportedly targeting the kinase activities of ATM and ATR.
CP-466722 is rapidly reversible potential ATM kinase inhibitor.
KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM.
Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50 of 3 nM and 0.17 (mu)M, respectively.