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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关于此项目
经验公式（希尔记法）:
C23H18Cl3FN4O3S
化学文摘社编号:
分子量:
555.84
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
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.
SMILES string
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
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
pale yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Target IC50: ~200 nM against ATM and ATR
Cell permeable: yes
Primary Target
ATM/ATR
ATM/ATR
Product does not compete with ATP.
Reversible: no
Disclaimer
Toxicity: Irritant (B)
General description
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.
Other Notes
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)
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_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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