118501
ATM/ATR Kinase Inhibitor
The ATM/ATR Kinase Inhibitor, also referenced under CAS 905973-89-9, controls the biological activity of ATM/ATR Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
ATM/ATR Kinase Inhibitor, CGK 733
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About This Item
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质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale yellow
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
Fc1c(cc(cc1)NC(=S)NC(NC(=O)C(c3ccccc3)c2ccccc2)C(Cl)(Cl)Cl)[N+](=O)[O-]
InChI
1S/C23H18Cl3FN4O3S/c24-23(25,26)21(30-22(35)28-16-11-12-17(27)18(13-16)31(33)34)29-20(32)19(14-7-3-1-4-8-14)15-9-5-2-6-10-15/h1-13,19,21H,(H,29,32)(H2,28,30,35)
InChI key
HLCDNLNLQNYZTK-UHFFFAOYSA-N
一般描述
A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC50 = ~200 nM) without significant effect against other PIKK family members (PI 3-K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI 3-K/PDK1/Akt signaling pathway.
A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC50 ~ 200 nM) without significant effect against other PIKK family members (PI3K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53 (ERK, CK1, Cdk2, JNK, PKC, CAK, Chk1, PKR, and p38). Shown to reverse senescence in human primary BJ and HMEC cells. Unlike LY 294002 (Cat. No. 440202 and 440204), this inhibitor does not interfere with cellular PI3K-PDK1-Akt signaling pathway.
生化/生理作用
Cell permeable: yes
Primary Target
ATM/ATR
ATM/ATR
Product does not compete with ATP.
Reversible: no
Target IC50: ~200 nM against ATM and ATR
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Goldstein, M., et al. 2008. Toxicol. Appl. Pharmacol.in press.
Crescenzi, E., et al. 2008. Clin. Cancer Res.14, 1877.
Cruet-Hennequart, S., et al. 2008. DNA Repair7, 582.
Won, J., et al. 2006. Nat. Chem. Biol.2, 369. (RETRACTED)
Crescenzi, E., et al. 2008. Clin. Cancer Res.14, 1877.
Cruet-Hennequart, S., et al. 2008. DNA Repair7, 582.
Won, J., et al. 2006. Nat. Chem. Biol.2, 369. (RETRACTED)
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Filippo Caraci et al.
Current neuropharmacology, 21(9), 2006-2018 (2023-04-07)
Ectopic cell cycle reactivation in neurons is associated with neuronal death in Alzheimer's disease. In cultured rodent neurons, synthetic β-amyloid (Aβ) reproduces the neuronal cell cycle re-entry observed in the Alzheimer's brain, and blockade of the cycle prevents Aβ-induced neurodegeneration.
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