5.33464
AMPK Activator, COH-SR4
Synonym(s):
AMPK Activator, COH-SR4, SR4
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About This Item
Empirical Formula (Hill Notation):
C13H8Cl4N2O
CAS Number:
Molecular Weight:
350.03
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
solid
potency
5-11 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 50 mg/mL
Quality Level
General description
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).
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.
Biochem/physiol Actions
Cell permeable: yes
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
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.
Figarola, J. L., et al. 2013. Int. J. Mol. Med.31, 1166.
Singhal, S. S., et al. 2012. Biochem. Pharm.84, 1419.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
flash_point_f
Not applicable
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_c
Not applicable
Regulatory Information
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