Molecular Weight(MW): 360.39
A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
Cited by 6 Publications
4 Customer Reviews
Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT.
Cancer Res 2014 74(1), 298-308. A-769662 purchased from Selleck.
Eight- to 10-week-old Ldlr-/- mice fed a standard laboratory chow were fasted overnight, fed at 07:00 h for 2 h, and refasted at 09:00 h. Intraperitoneal injection of vehicle, GW1516 (3 mg/kg), or A-769662 (30 mg/kg) (n = 6/group) occurred at the beginning of the refasting period at 09:00 h. Immunoblots of AMPK and ACC in freeze-clamped liver lysates 90 min postinjection. Representative immunoblots with quantitations are shown. Asterisk (*) indicates significant difference between vehicle and treatment; Student's paired t-test (P < 0.05).
J Lipid Res 2014 55(7), 1254-1266. A-769662 purchased from Selleck.
Concentration-dependent effect of synthetic AMPK stimulator, A-769662, applied for 10 min on phosphorylated α subunit of AMPK. AMPK inhibitor (compound C, CC) was added to some samples at 10 uM. **p < 0.01, ***p < 0.001 vs. sample without A-769662 by ANOVA and Tukey post hoc test.
Pharmacol Res 2014 81, 34-43. A-769662 purchased from Selleck.
Cultured PANC-1 pancreatic cancer cells were treated with vehicle (DMSO, 1%), 10 uM of belinostat (BS, for 2 h, 4 h and 6 h) or A-769662 (10 uM, 2 h), phospho- and total AMPK and ACC were detected by western blot, tubulin (loading control) was also tested. AMPK and ACC phosphorylation was quantified as described.
Biochem Biophys Res Commun 2013 437(1), 1-6. A-769662 purchased from Selleck.
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Choose Selective AMPK Inhibitors
|Description||A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.|
A-769662 stimulates partially purified rat liver AMPK with EC50 with 0.8 μM. A-769662 activates AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 mM, 1.9 mM, or 1.1 mM, respectively. A 4 hours treatment of primary rat hepatocytes with A-769662 dose-dependently increases ACC phosphorylation, which correlated inhibition of fatty acid synthesis with IC50 of 3.2 μM. A-769662 also inhibits fatty acid sythesis in mouse hepatocytes with IC50 with 3.6 μM  A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP.  A-769662 inhibits proteasomal function by an AMPK-independent mechanism. A-769662 affects the in vitro activity of purified 26S proteasomes but not the in vitro activity of purified 20S proteasomes. A-769662 has toxic effects on MEF cells.  A recent research shows A-769662 inhibited cell proliferation and DNA synthesis. 
|In vivo||Short-term treatment of normal Sprague Dawley rats with A-769662 decreases liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreases hepatic expression of PEPCK, G6Pase, and FAS, lowers plasma glucose by 40%, reduced body weight gain and significantly decreases both plasma and liver triglyceride levels. |
96-well AMPK assay:AMPK activity is measured by monitoring phosphorylation of the SAMS peptide substrate (20 mM in standard assays and 100 mM in additivity assays) following a previously described protocol (Anderson et al., 2004). To determine whether A-769662-induced AMPK activation occurs in a reversible manner, AMP or A-769662 are preincubated with rat liver AMPK for 10 minutes at 20 times standard assay concentrations prior to dilution and measurement of AMPK activity.
|In vitro||DMSO||72 mg/mL (199.78 mM)|
|In vivo||1% DMSO+30% polyethylene glycol+1% Tween 80||30 mg/mL|
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