Biochem/physiol Actions
Reversible: yes
Product competes with ATP.
Target IC50: 17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK
Primary TargetHuman Bruton′s Tyrosine Kinase (BTK)
Cell permeable: yes
General description
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton's Tyrosine Kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s tyrosine kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
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: Standard Handling (A)
This product has met the following criteria: