Pular para o conteúdo
Merck
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Key Documents

118502

Sigma-Aldrich

ATM Kinase Inhibitor

InSolution, ≥95%

Sinônimo(s):

InSolution ATM Kinase Inhibitor

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About This Item

Fórmula empírica (Notação de Hill):
C21H17NO3S2
Peso molecular:
395.49
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥95% (HPLC)

forma

liquid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
desiccated (hygroscopic)
protect from light

Condições de expedição

wet ice

temperatura de armazenamento

−20°C

Descrição geral

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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

forma física

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

Reconstituição

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

Outras notas

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.

Informações legais

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

Código de classe de armazenamento

10 - Combustible liquids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Ponto de fulgor (°C)

87 °C - closed cup - (Dimethylsulfoxide)


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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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