Potent and selective ATM kinase inhibitor IC50s= 13, 2500, 9300, 16600, >100000 and >100000 nM for ATM, DNA-PK, mTOR, PI 3-kinase, PI 4-K and ATR respectively.1Decreases viability of MCF-7, A549 and HCT116 cells and decreases p21CIP1 levels in vitro.2 Disruption of ATM signaling in primary A-T fibroblasts leads to dysregulation of ribonucleotide reductase and increase resistance to inhibitors of mitochondrial respiration and translation.3 Sensitizes radio-resistant cancer cells.4Provides neuroprotection against H2O2-induced cell damage.5 ATM、DNA-PK、mTOR、PI 3-激酶、PI 4-K和ATR的有效选择性ATM激酶抑制剂IC50s分别为13、2500、9300、16600、>100000和>100000 nM。 1体外降低MCF-7、A549、HCT116细胞活力,降低p21CIP1水平 在原代A-T成纤维细胞中ATM信号的中断会导致核糖核苷酸还原酶的失调,并增加对线粒体呼吸和翻译抑制剂的耐药性 使耐辐射的癌细胞增敏。 4对h2o2诱导的细胞损伤提供神经保护。
References/Citations:
1) Hickson et al. (2004), Identification and characterization of a novel and specific inhibitor of the ataxia-telangiectasia mutated kinase ATM; Cancer Res., 64 9152 2) Crescenzi et al. (2008), Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy; Clin. Cancer Res. 14 1877 3) Eaton et al. (2007), Ataxia-telangiectasia mutated kinase regulates ribonucleotide reductase and mitochondrial homeostasis; J. Clin. Invest., 117 2723 4) Zhang et al. (2015) The ATM inhibitor KU55933 sensitizes radioresistant bladder cancer cells with DAB2IP gene defect; Int. J. Radiat. Biol., 91 368 5) Chwastek et al. (2017) The ATM kinase inhibitor KU-55933 provides neuroprotection against hydrogen peroxide-induced cell damage via a yH2AX/p-p53/caspase-3-independent mechanism: Inhibition of calpain and cathepsin D; Int. J. Biochem. Cell Biol. 87 38
CAS:
587871-26-9
Catalog Number:
10-1518
Activity:
ATM Kinase Inhibitor
Chemical Name:
2-(4-Morpholinyl)-6-(1-thiamthrenyl)-4H-pyran-4-one
Molecular Weight:
395.5
Molecular Formula:
C21H17NO3S2 Solubility:
Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 20 mg/ml)
Physical Properties:
Tan solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Shipping Code:
RT
更多产品咨询联系 上海惠诚生物 联系人:任荣 电话:18017273415