ERK Inhibitor II, FR180204

A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC₅₀ = 510 nM and 330 nM; K_i = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC₅₀ = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC₅₀ of 3.1 µM). ERK Inhibitor II, Negative Control (Cat. No. 328008 ) and the solid form of this compound (Cat. No. 328007 ) are also available..

A cell-permeable pyrazolopyridazinamine that acts as a potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC₅₀ = 510 nM and 330 nM; K_i = 310 nM and 140 nM, respectively). Exhibits ~20-fold greater selectivity over p38α (IC₅₀ = 10 µM) and shows little activity towards IKKα, MEK1, MKK4, PDGFRα, PKCα, Src, and Syk even at concentrations as high as 30 µM. Shown to inhibit TGF-β−induced AP-1 activation in Mv1Lu epithelial cells (IC₅₀ of 3.1 µM). ERK Inhibitor II, Negative Control is also available (Cat. No. 328008).

Packaged under inert gas

A 10 mM (500 µg/153 µl) solution of ERK Inhibitor II, FR180204 (Cat. No. 328007) in DMSO.

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

Toxicity: Irritant (B)