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. Also available as a 10 mM solution in DMSO (Cat. No. 171261).

Legal Information

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

Other Notes

Hao, J., et al. 2010. ACS Chem.Biol.5, 245.Yu, P.B., et al. 2008. Nat. Chem. Biol4, 33.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

Packaged under inert gas

1, 5, 10 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)