Merck, 565851-50MG, SHP1/2 PTPase Inhibitor, NSC-87877

General description
A cell-permeable 7-aza-8-hydroxyquinoline compound that acts as a potent, catalytic site-targeting inhibitor of SHP-1 and SHP-2 protein tyrosine phosphatases (IC₅₀ = 355 nM and 318 nM, respectively). It inhibits PTP1B and HePTP with less potency (IC₅₀ = 1.69 µM and 7.75 µM, respectively) and exhibits >200-fold selectivity over DEP1, CD45, and LAR. Shown to inhibit both basal and stimulated SHP-2 activity in HEK293 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
SHP1/2 PTPase
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 355 nM and 318 nM against SHP-1 and SHP-2 protein tyrosine phosphatases, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chen, L., et al. 2006. Mol. Pharmacol.70, 562.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)