Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Target IC₅₀: 100 µM and 10 µM against insulin receptor tyrosine kinase and insulin-stimulated glucose oxidation in isolated rat adipocytes, respectively

Primary Targettyrosine kinase

Cell permeable: yes

General description

A cell-permeable analog of HNMPA. Inhibits insulin receptor tyrosine kinase (IC₅₀ = 100 mM) and insulin-stimulated glucose oxidation in isolated rat adipocytes (IC₅₀ = 10 µM). Also reported to inhibit tyrosine autophosphorylation of the human insulin receptor (IC₅₀ = 200 µM). It has no effect on PKA (at concentrations up to 1 mM) or PKC (at concentrations up to 420 µM).

A cell-permeable analog of HNMPA that yields the parent compound upon cleavage by cytosolic esterases. Inhibits insulin receptor tyrosine kinase (IC₅₀ = 100 µM) and insulin-stimulated glucose oxidation in isolated rat adipocytes (IC₅₀ = 10 µM). Also reported to inhibit tyrosine autophosphorylation of the human insulin receptor (IC₅₀ = 200 µM).

Legal Information

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

Other Notes

Baltensperger, K., et al. 1992. Proc. Natl. Acad. Sci. USA89, 7885.Saperstein, R., et al. 1989. Biochemistry28, 5694.

Packaging

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)