Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Cell permeable: yes

Target IC₅₀: 25.1, 148, and 234.6 nM, against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity, respectively

Primary TargetAMPK

EC100 = 2.5 µM against BMP pathway-dependent dorsoventral development; EC50 = 5 µM against VEGF signaling-dependent intersomitic vessel formation in zebrafish embryo in vivo

General description

A cell-permeable pyrrazolopyrimidine compound that inhibits against KDR/VEGFR2, ALK2/BMPR-I, AMPK kinase activity (IC₅₀ = 25.1, 148, and 234.6 nM, respectively), while exhibiting much reduced or little effect toward ALK5/TGFβR-I, ZAPK, Syk, PKCθ, PKA, or JAK3. Shown to block both BMP pathway-dependent dorsoventral development (EC₁₀₀ = 2.5 µM) and VEGF signaling-dependent intersomitic vessel formation (EC₅₀ = 5 µM) in zebrafish embryo in vivo. Commonly used in combination with AMPK activators AICAR (Cat. No. 123040) and/or Metformin (Cat. No. 317240) for studying AMPK-dependent cellular events in vitro and physiological responses in animals in vivo.

Legal Information

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

Other Notes

Hao, J., et al. 2010. ACS Chem.Biol.5, 245.Kim, E.K., et al. 2004. J. Biol. Chem.279, 19970.Lee, M., et al. 2003. J. Biol. Chem.278, 39653.Inoki, K., et al. 2003. Cell115, 577.Fryer, L.G., 2002. FEBS Lett.531, 189.Zhou, G., et al. 2001. J. Clin. Invest.108, 1167.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

Supplied as a 10 mM (1 mg/250 µl) solution of AMPK Inhibitor, Compound C (Cat. No. 171260) in DMSO.

Reconstitution

Following initial use, aliquot and freeze (-20°C). Once opened, stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Irritant (B)