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Formula | C20H12N2O3S |
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Molecular Weight | 360.39 | CAS No. | 844499-71-4 | ||||
Solubility (25°C)* | In vitro | DMSO | 72 mg/mL (199.78 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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. | ||||
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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] |
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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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Data from [Cancer Res, 2014, 74(1), 298-308]
Data from [Data independently produced by Pharmacol Res, 2014, 81, 34-43]
Data from [Data independently produced by J Lipid Res, 2014, 55(7), 1254-1266]
Data from [Data independently produced by Biochem Biophys Res Commun, 2013, 437(1), 1-6]
Nuclear PD-L1 compartmentalization suppresses tumorigenesis and overcomes immunocheckpoint therapy resistance in mice via histone macroH2A1 [ J Clin Invest, 2024, 134(22)e181314] | PubMed: 39545415 |
Hypoxanthine phosphoribosyl transferase 1 metabolizes temozolomide to activate AMPK for driving chemoresistance of glioblastomas [ Nat Commun, 2023, 14(1):5913] | PubMed: 37737247 |
Hypoxanthine phosphoribosyl transferase 1 metabolizes temozolomide to activate AMPK for driving chemoresistance of glioblastomas [ Nat Commun, 2023, 14(1):5913] | PubMed: 37737247 |
Pathogenesis-related protein 1 suppresses oomycete pathogen by targeting against AMPK kinase complex [ J Adv Res, 2023, 43:13-26] | PubMed: 36585103 |
A subset of VEGFR-TKIs activates AMPK in LKB1-mutant lung cancer [ Cancer Sci, 2023, 114(4):1651-1662] | PubMed: 36459496 |
A subset of VEGFR-TKIs activates AMPK in LKB1-mutant lung cancer [ Cancer Sci, 2023, 114(4):1651-1662] | PubMed: 36459496 |
Loss of Lactate/Proton Monocarboxylate Transporter 4 Induces Ferroptosis via the AMPK/ACC Pathway and Inhibition of Autophagy on Human Bladder Cancer 5637 Cell Line [ J Oncol, 2023, 2023:2830306] | PubMed: 36718218 |
Discovery of a natural small-molecule AMP-activated kinase activator that alleviates nonalcoholic steatohepatitis [ Mar Life Sci Technol, 2023, 5(2):196-210] | PubMed: 37275542 |
Identification of purine biosynthesis as an NADH-sensing pathway to mediate energy stress [ Nat Commun, 2022, 13(1):7031] | PubMed: 36396642 |
AMPK regulates homeostasis of invasion and viability in trophoblasts by redirecting glucose metabolism: Implications for pre-eclampsia [ Cell Prolif, 2022, e13358.] | PubMed: 36480593 |
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