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A-769662

Catalog No. T2468 CAS 844499-71-4

Synonyms: A 769662

A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).

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A-769662, CAS 844499-71-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 145.00
50 mg	In stock	$ 270.00
100 mg	In stock	$ 489.00
500 mg	In stock	$ 1,070.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.58%

Purity: 98.72%

Purity: 98.23%

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Description	A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).
Targets&IC50	AMPK:0.8 μM(EC50)
In vitro	In ob/ob mice, A-769662 (30 mg/kg, b.i.d.) effectively reduces the hepatic expression of PEPCK, G6Pase, and FAS, decreases plasma glucose levels, and lowers triglyceride levels in both plasma and liver, thereby mitigating weight gain.
In vivo	A-769662 activates AMPK, purified from various tissues and species, in a dose-dependent manner, demonstrated across purified rat liver (EC50=0.8 μM), rat heart (EC50=2.2 mM), rat muscle (EC50=1.9 mM), and human embryonic kidney cells (HEKs) (EC50=1.1 mM). In hepatocytes, A-769662 enhances ACC phosphorylation and inhibits fatty acid synthesis, with IC50 values of 3.2 μM in primary rat hepatocytes and 3.6 μM in mouse hepatocytes. The activation of AMPK by A-769662 involves preventing the dephosphorylation at Thr-172 and structural modulation. Furthermore, A-769662 inhibits the in vitro activity of the purified 26S proteasome, as well as cell proliferation and DNA synthesis.
Kinase Assay	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.
Cell Research	Cell viability of MEF cells treated or not with A-769662 is performed as follows: cells are harvested by trypsinization and incubated with 0.5 mg/mL RNase and 50 μg/mL propidium iodine at room temperature in the dark; cell viability is analyzed by flow cytometry using a FACScanto flow cytometer, using an excitation laser at 488 nm and a propidium iodine fluorescence detection at 600 nm. To determine the proportion of cells in each phase of the cell cycle, cells are harvested by trypsinization, collected by centrifugation, washed in PBS and fixed overnight in 80% ethanol at -20 °C. Subsequently, these fixed cells are centrifuged to remove the fixative and incubated for 20 minutes in the dark at room temperature in PBS containing 0.5 mg/mL RNase and 50 μg/mL propidium iodine. Flow cytometry analysis is performed as above. The proportion of cells in G1, S, and G2 is determined using the MODFIT program. Cell culture pictures are taken at the indicated times using a camera coupled to an inverted microscope with a 20 × objective. (Only for Reference)

Synonyms	A 769662
Molecular Weight	360.39
Formula	C20H12N2O3S
CAS No.	844499-71-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3.6 mg/mL (10 mM)

DMSO: 36 mg/mL (100 mM)

References and Literature

1. Cool B, et al, Cell Metab, 2006, 3(6), 403-416. 2. Sanders MJ, J Biol Chem, 2007, 282(45), 32539-32548. 3. Moreno D, et al, FEBS Lett, 2008, 583(17), 2650-2654. 4. Pevton KJ, et al, J Pharmacol Exp Ther, 2012, Jun 13. 5. Lu X Y, Shi X J, Hu A, et al. Feeding induces cholesterol biosynthesis via the mTORC1–USP20–HMGCR axis[J]. Nature. 2020, 588(7838): 479-484.

Citations

1. Lu X Y, Shi X J, Hu A, et al. Feeding induces cholesterol biosynthesis via the mTORC1–USP20–HMGCR axis. Nature. 2020, 588(7838): 479-484.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Lung Cancer Compound Library Oxidation-Reduction Compound Library Anti-Cancer Metabolism Compound Library Cancer Cell Differentiation Compound Library Anti-Hypertension Compound Library Anti-Breast Cancer Compound Library Epigenetics Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

A-769662 844499-71-4 Chromatin/Epigenetic Metabolism PI3K/Akt/mTOR signaling AMPK Fatty Acid Synthase Inhibitor inhibit AMP-activated protein kinase A769662 A 769662 inhibitor

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