Biochem/physiol Actions

Cell permeable: yes

General description

AMPK Activator, COH-SR4, is a cell permeable AMPK activator that acts upstream of AMPK. Increases AMPK phosphorylation and activation in preadipocytes and cancer cell lines.

A cell permeable, orally bioavailable bis(dichlorophenyl)urea that acts as an AMPK activator via possibly targeting upstream of AMPK. Shown to increase AMPK phosphorylation and activation in multiple preadipocytes and cancer cell lines dose-dependently. Inhibits glutathione S transferase (GST) activity and induces G2/M phase cell cycle arrest in multiple melanoma cells (IC₅₀ = 5-11 µM). Effectively inhibits tumor burden, decreases angiogenesis marker CD31 and proliferation marker Ki67, and increases pAMPK levels in vivo (4 mg/kg p.o., mouse) without obvious toxicity. Displays similar anti-cancer effects in lung cancer models both in vitro and in vivo. In addition, shown to down-regulate key proteins involved in fatty acid synthesis and inhibits adipocyte differentiation via AMPK activation in 3T3-L1 obesity model cells (IC₅₀ = ~1.5 µM).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

A cell permeable, orally bioavailable bis(dichlorophenyl)urea that acts as an AMPK activator via possibly targeting upstream of AMPK. Shown to increase AMPK phosphorylation and activation in multiple preadipocytes and cancer cell lines dose-dependently. Inhibits glutathione S transferase (GST) activity and induces G2/M phase cell cycle arrest in multiple melanoma cells (IC₅₀ = 5-11 µM). Effectively inhibits tumor burden, decreases angiogenesis marker CD31 and proliferation marker Ki67, and increases pAMPK levels in vivo (4 mg/kg p.o., mouse) without obvious toxicity. Displays similar anti-cancer effects in lung cancer models both in vitro and in vivo. In addition, shown to down-regulate key proteins involved in fatty acid synthesis and inhibits adipocyte differentiation via AMPK activation in 3T3-L1 obesity model cells (IC₅₀ = ~1.5 µM).

Legal Information

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

Other Notes

Singhal, S. S., et al. 2013. Biochem. Pharm.86, 1664. Figarola, J. L., et al. 2013. Int. J. Mol. Med.31, 1166. Singhal, S. S., et al. 2012. Biochem. Pharm.84, 1419.

Packaging

10 mg in Glass bottle

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)