Biochem/physiol Actions

Secondary TargetALK 5 auto phosphorylation (IC₅₀ = 4 nM)

Primary TargetALKS binding

Product competes with ATP.

Cell permeable: yes

General description

A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of TGF-β type I receptor (ALK5; IC₅₀ = 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation, and TGF-β cellular assay in HepG2 cells, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK (IC₅₀ >16 µM).

A cell-permeable naphthyridinyl pyrazolo compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β type I receptor (ALK5; IC₅₀ = 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation and TGF-β cellular assay in HepG2 cells, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK at IC₅₀ >16 µM. Also available as a 50 mM solution in DMSO (Cat. No. 508158).

Legal Information

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

Other Notes

Gellibert, F., et al. 2004. J. Med. Chem.47, 4494.Ichida, J. K., et al. 2009. Cell Stem Cell 5, 491.

Packaging

Packaged under inert gas

2 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)