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)
This product has met the following criteria to qualify for the following awards: