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Merck
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Key Documents

118502

Sigma-Aldrich

ATM Kinase Inhibitor

InSolution, ≥95%

Synonyme(s) :

InSolution ATM Kinase Inhibitor

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About This Item

Formule empirique (notation de Hill):
C21H17NO3S2
Poids moléculaire :
395.49
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥95% (HPLC)

Forme

liquid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
desiccated (hygroscopic)
protect from light

Conditions d'expédition

wet ice

Température de stockage

−20°C

Description générale

A cell-permeable disubstituted pyranone compound that acts as a potent and ATP-competitive inhibitor of ATM kinase (IC50 = 13 nM; Ki = 2.2 nM). Displays excellent selectivity over other PIKK family kinases (IC50 = 2.5, 9.3, 16.6 µM for DNA-PK, mTOR, PI 3-K, respectively; IC50 >100 µM for PI 4-K and ATR) and exhibits little activity towards a panel of 60 other kinases even at concentrations as high as 10 µM. Inhibits ATM-dependent cellular protein phosphorylation following ionizing radiation (IR) and sensitizes cells with wild-type ATM, but not mutant ATM, to the cytotoxic effects of IR and DNA-damaging agents.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Forme physique

A 10 mM (2 mg/506 µl) solution of ATM Kinase Inhibitor (Cat. No. 118500) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C).

Autres remarques

Pereg, Y., et al. 2005. Proc. Natl. Acad. Sci. USA102, 5056.
Lau, A., et al. 2005. Nat. Cell Biol.7, 493.
Hickson, I., et al. 2004. Cancer Res.64, 9152.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Code de la classe de stockage

10 - Combustible liquids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Point d'éclair (°C)

87 °C - closed cup - (Dimethylsulfoxide)

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Alan Lau et al.
Nature cell biology, 7(5), 493-500 (2005-04-19)
Chemotherapy that is used to treat human immunodeficiency virus type-1 (HIV-1) infection focuses primarily on targeting virally encoded proteins. However, the combination of a short retroviral life cycle and high mutation rate leads to the selection of drug-resistant HIV-1 variants.
Yaron Pereg et al.
Proceedings of the National Academy of Sciences of the United States of America, 102(14), 5056-5061 (2005-03-25)
Maintenance of genomic stability depends on the DNA damage response, an extensive signaling network that is activated by DNA lesions such as double-strand breaks (DSBs). The primary activator of the mammalian DSB response is the nuclear protein kinase ataxia-telangiectasia, mutated
Ian Hickson et al.
Cancer research, 64(24), 9152-9159 (2004-12-18)
The serine/threonine protein kinase ATM signals to cell cycle and DNA repair components by phosphorylating downstream targets such as p53, CHK2, NBS1, and BRCA1. Mutation of ATM occurs in the human autosomal recessive disorder ataxia-telangiectasia, which is characterized by hypersensitivity

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