Biochem/physiol Actions

Primary TargetJAK2 autophosphorylation

Reversible: yes

Product does not compete with ATP.

Cell permeable: yes

General description

A cell-permeable hexabromocyclohexane compound that interacts with a solvent-accessible pocket near the activation loop of JAK2 and acts as a specific, reversible, and direct inhibitor of JAK2 autophosphorylation (maximal inhibition at 50 µM in BSC-40 cells overexpressing JAK2). Reduces growth hormone-mediated JAK2 activation in γ2A cells that stably express growth hormone receptor and JAK2. Does not block EGFR autophosphorylation in murine fibroblasts.

A cell-permeable, specific, reversible, and direct inhibitor of JAK2 autophosphorylation (maximal inhibition at 50 µM in BSC-40 cells overexpressing JAK2 that interacts with a solvent-accessible pocket near the activation loop of JAK2. Reduces growth hormone-mediated JAK2 activation in γ2A cells that stably express growth hormone receptor and JAK2. Does not block EGFR autophosphorylation in murine fibroblasts.

Legal Information

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

Other Notes

Sandberg, E.M., et al. 2005. J. Med. Chem.48, 2526.

Packaging

Packaged under inert gas

25 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)