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A769662

(CAS No:844499-71-4)
A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
CAS No:844499-71-4
Molecular Weight(MW):360.39
Purity:98.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 844499-71-4
Molecular formula(MF) C20H12N2O3S
Molecular Weight(MW): 360.39
Alias A 769662
Solubility
In vitro DMSO 72 mg/mL (199.78 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
Biological Activity
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.
Targets
AMPK [1]
(Cell-free assay)		 Fatty acid synthesis [1]
(Cell-free assay)
0.8 μM(EC50) 3.2 μM
In vitro

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 [1] A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. [2] 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. [3] A recent research shows A-769662 inhibited cell proliferation and DNA synthesis. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse hepatocytes Function assay 1 mM DMSO inhibits fatty acid synthesis with IC50 of 3.6 μM 16753576
rat hepatocytes Function assay 1 mM DMSO inhibits fatty acid synthesis with IC50 of 3.6 μM 16753576
HEK293 Kinase assay 200 μM DMSO activates endogenous AMPK 17728241
CCL13 Kinase assay 200 μM DMSO activates endogenous AMPK 17728241
MEFs Function assay 300 μM DMSO inhibits proteasomal function by an AMPK-independent mechanism 18593584
epididymal clear cells Function assay 200 μM DMSO inhibits the pH-mediated V-ATPase accumulation at the apical membrane 19211918
3T3-L1 Function assay 1.2 mM DMSO inhibits 3T3-L1 Adipogenesis 19483304
3T3-L1 Function assay 1.2 mM DMSO inhibits the Expression of AdipogenesisRelated Transcription Factors and Markers 19483304
3T3-L1 Function assay 1.2 mM DMSO inhibits Mitotic Clonal Expansion 19483304
3T3-L1 cytotoxicity assay 1.2 mM DMSO decreases Cell Viability 19483304
3T3-L1 Kinase assay 1.2 mM DMSO activates AMPK 19483304
L6 skeletal muscle cells Function assay 250 μM DMSO activates AMPK signaling pathways 19828836
L6 skeletal muscle cells Function assay 250 μM DMSO inhibits the Na+-K+-ATPase transport activity and cell surface abundance 19828836
MDA-MB231 Apoptosis assay 400 μM DMSO sensitizes human breast cancer cell lines to TRAIL-induced apoptosis 19896469
BT474 Apoptosis assay 400 μM DMSO sensitizes human breast cancer cell lines to TRAIL-induced apoptosis 19896469
MCF7 Apoptosis assay 400 μM DMSO sensitizes human breast cancer cell lines to TRAIL-induced apoptosis 19896469
Mesenchymal stem cells Kinase assay 10 µM DMSO induces a robust and sustained AMPK activation 24104879
Mesenchymal stem cells cytotoxicity assay 100 µM DMSO decreases the MSC proliferation 24104879
MG-63 cytotoxicity assay 10 µM DMSO inhibits H2O2-Induced Osteoblast Cell Death 24960362
MC3T3-E1 cytotoxicity assay 10 µM DMSO inhibits H2O2-Induced Osteoblast Cell Death 24960362
MG-63 Apoptosis assay 10 µM DMSO suppresses H2O2-Induced Osteoblast Cell Apoptosis 24960362
MC3T3-E1 Apoptosis assay 10 µM DMSO suppresses H2O2-Induced Osteoblast Cell Apoptosis 24960362
MG-63 Function assay 10 µM DMSO alleviates ROS accumulation and ATP depletion caused by H2O2 24960362
MC3T3-E1 Function assay 10 µM DMSO alleviates ROS accumulation and ATP depletion caused by H2O2 24960362
MG-63 Function assay 10 µM DMSO facilitates H2O2-induced autophagy activation 24960362
MC3T3-E1 Function assay 10 µM DMSO facilitates H2O2-induced autophagy activation 24960362
PC3 Kinase assay 100 µM DMSO upregulates the levels of AMPK and ACC phosphorylation 25594043
PC3M Kinase assay 100 µM DMSO upregulates the levels of AMPK and ACC phosphorylation 25594043
PC3 Function assay 100 µM DMSO induces PI3K/mTOR pathways 25594043
PC3M Function assay 100 µM DMSO induces PI3K/mTOR pathways 25594043
PC3 Growth inhibitory assay 100 µM DMSO suppresses proliferation 25594043
PC3M Growth inhibitory assay 100 µM DMSO suppresses proliferation 25594043
MC3T3-E1 Kinase assay 10 μM DMSO induces significant AMPK activation 26891866
MC3T3-E1 Growth inhibitory assay 10 μM DMSO inhibits Dex-induced osteoblast cell death 26891866
MC3T3-E1 Function assay 10 μM DMSO inhibits Dex-induced oxidative stress 26891866

... Click to View More Cell Line Experimental Data
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. [1]
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