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220488

Sigma-Aldrich

Chk2 Inhibitor, PV1019

The Chk2 Inhibitor, PV1019 controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sinónimos:

Chk2 Inhibitor, PV1019, NSC 744039

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About This Item

Fórmula empírica (notación de Hill):
C18H17N7O3
Peso molecular:
379.37
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

Ensayo

≥95% (HPLC)

Formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
desiccated (hygroscopic)
protect from light

color

orange

solubilidad

DMSO: 5 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

−20°C

Descripción general

A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50 = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50 = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50<10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/- cultures.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther.331, 816.

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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