CHK2 INHIBITOR II

Code: 220486-1MG D2-231

Biochem/physiol Actions

Target Ki: 37 nM inhibiting Chk2

Reversible: yes

Product competes with ATP.

Primary TargetChk2

Ki = 37 nM inhibitin...


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€219.50 1MG
€269.99 inc. VAT

Biochem/physiol Actions

Target Ki: 37 nM inhibiting Chk2

Reversible: yes

Product competes with ATP.

Primary TargetChk2

Ki = 37 nM inhibiting Chk2.EC50 = 3 µM and 7.6 µM in rescuing both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis

Cell permeable: yes

General description

A cell-permeable, potent, reversible and ATP-competitive inhibitor of Chk2 (checkpoint kinase 2; IC50 = 15 nM; Ki = 37 nM). Displays ~1,000-fold greater selectivity for Chk2 compared to Cdk1/cyclin B and CK1 (IC50 = 12 µM and 17 µM, respectively) and only weakly affects the activities of a panel of 31 kinases (﹤25% inhibition at 10 µM), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC50 of 3 µM and 7.6 µM, respectively.

A cell-permeable and reversible benzimidazolo compound that acts as a potent and ATP-competitive inhibitor of Chk2 with an IC50 of 15 nM and a Ki of 37 nM. Displays ~ 1,000-fold greater selectivity over Cdk1/B and CK1 (IC50 = 12 M and 17 M, respectively) and only weakly affects the activities of a panel of 31 kinases (﹤25% inhibition at 10 M), including Chk1. Shown to rescue both peripheral CD4+ and CD8+ T-cells from γ-irradiation-induced apoptosis with an EC50 of 3 M and 7.6 M, respectively. Also available as a 25 mM solution in DMSO (Cat. No. 220491).

Legal Information

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

Other Notes

Arienti, K. L., et al. 2005. J. Med. Chem.48, 1873.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)

assay≥95% (HPLC)
colorpale yellow
formsolid
manufacturer/tradenameCalbiochem®
potency15 nM IC50
Quality Level100
shipped inambient
solubilityDMSO: 5 mg/mL
storage conditionprotect from light, OK to freeze
storage temp.2-8°C
Cas Number516480-79-8
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