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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Tamaño de envase
SKU
Disponibilidad
Precio
10 mg
220488-10MG
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OK to freeze, desiccated (hygroscopic), protect from light
color
orange
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther.331, 816.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
OK to freeze, protect from light, desiccated (hygroscopic)
storage condition
OK to freeze, protect from light
storage condition
OK to freeze, protect from light
storage condition
OK to freeze, protect from light
Clase de almacenamiento
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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