Biochem/physiol Actions

Primary TargetPIM1 kinase

Reversible: yes

Product competes with ATP.

Target IC₅₀: 340 nM against PIM1 kinase

Cell permeable: yes

General description

A cell-permeable flavanol compound that acts a potent, ATP-competitive, and reversible inhibitor of PIM1 kinase (IC₅₀ = 340 nM). Exhibits ≥7-fold selectivity over 8 other kinases tested, including PIM2 (IC₅₀ = 3.45 µM), and little activity toward c-Abl even at concentrations as high as 200 µM. Inhibits cellular BAD phosphorylation (IC₅₀ = 5.5 µM) and induces growth arrest (ED₅₀ = 3.8 µM) in PIM1-expressing RWPE2 cells.

Legal Information

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

Other Notes

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Holder, S., et al. 2007. Mol. Cancer Ther.6, 163.

Packaging

Packaged under inert gas

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: Toxic & Carcinogenic / Teratogenic (G)