220488
Chk2 Inhibitor, PV1019
The Chk2 Inhibitor, PV1019 controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonim(y):
Chk2 Inhibitor, PV1019, NSC 744039
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About This Item
Wzór empiryczny (zapis Hilla):
C18H17N7O3
Masa cząsteczkowa:
379.37
Kod UNSPSC:
12352200
NACRES:
NA.77
Polecane produkty
Poziom jakości
Próba
≥95% (HPLC)
Postać
solid
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
desiccated (hygroscopic)
protect from light
kolor
orange
rozpuszczalność
DMSO: 5 mg/mL
Warunki transportu
ambient
temp. przechowywania
−20°C
Opis ogólny
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.
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.
Opakowanie
Packaged under inert gas
Ostrzeżenie
Toxicity: Standard Handling (A)
Rekonstytucja
Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Inne uwagi
Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther.331, 816.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
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