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220488 Chk2 Inhibitor, PV1019 - Calbiochem

220488
Purchase on Sigma-Aldrich

Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical Formula
C₁₈H₁₇N₇O₃

Products

Numero di catalogoConfezionamento Qtà/conf
220488-10MG Bottiglia di vetro 10 mg
Description
OverviewA 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.
Catalogue Number220488
Brand Family Calbiochem®
SynonymsNSC 744039
References
ReferencesJobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331, 816.
Product Information
FormOrange solid
Hill FormulaC₁₈H₁₇N₇O₃
Chemical formulaC₁₈H₁₇N₇O₃
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Chk2 Inhibitor, PV1019 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

Chk2 Inhibitor, PV1019 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
220488

Riferimenti bibliografici

Panoramica delle referenze
Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331, 816.
Scheda tecnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision30-August-2010 RFH
SynonymsNSC 744039
DescriptionA 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.
FormOrange solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₈H₁₇N₇O₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (5 mg/ml)
Storage -20°C
Hygroscopic
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesJobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331, 816.