A-769662

Catalog No.S2697

A-769662 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 210 In stock
USD 147 In stock
USD 270 In stock
USD 470 In stock

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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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NXPJfJBOTnWwY4Tpc44h[XO|YYm= MWexJI1O NVTuVZAyTE2VTx?= M1TsTIlvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP M3zQT|E3PzV|NUe2
rat hepatocytes MYjGeY5kfGmxbjDhd5NigQ>? MXWxJI1O M1TafmROW09? NFvUXHNqdmirYnn0d{Bn[XS2eTDhZ4llKHO7boTo[ZNqeyC5aYToJGlEPTBib3[gN{43KM7:TR?= MUKxOlc2OzV5Nh?=
HEK293 NFKxeHVMcW6jc3WgZZN{[Xl? M170flIxOCEQvF2= NGD2[ZhFVVOR NY\sXFZE[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> M13rWFE4PzJ6MkSx
CCL13 MX;LbY5ie2ViYYPzZZk> NEDoTGYzODBizszN MUHEUXNQ NWHOXmxD[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> NW\oNXBbOTd5MkiyOFE>
MEFs NED1bIlHfW6ldHnvckBie3OjeR?= MmDON|AxKM7:TR?= MnXySG1UVw>? MU\pcohq[mm2czDwdo91\WG|b33hcEBnfW6ldHnvckBjgSCjbjDBUXBMNWmwZHXw[Y5l\W62IH3lZ4hidmm|bR?= M2rGXVE5PTl|NUi0
epididymal clear cells NFL5NmRHfW6ldHnvckBie3OjeR?= NIjjUVUzODBizszN NVXGRlJkTE2VTx?= MmXibY5pcWKrdIOgeIhmKHCKLX3l[IlifGWmIG[tRXRR[XOnIHHjZ5VufWyjdHnvckBifCC2aHWgZZBq[2GuIH3lcYJz[W6n MUKxPVIyOTlzOB?=
3T3-L1 NHzDPY1HfW6ldHnvckBie3OjeR?= MYqxMlIhdU1? NF\yOZRFVVOR MmCxbY5pcWKrdIOgN3Q{NUxzIFHkbZBw\2WwZYPpdy=> MmPuNVk1QDN|MES=
3T3-L1 MmXhSpVv[3Srb36gZZN{[Xl? MlrjNU4zKG2P NH;hPWlFVVOR M2HQPYlvcGmkaYTzJJRp\SCHeIDy[ZN{cW:wIH;mJGFlcXCxZ3Xu[ZNqe1KnbHH0[YQhXHKjboPjdolxfGmxbjDGZYN1d3K|IHHu[EBO[XKtZYLz M1vIS|E6PDh|M{C0
3T3-L1 M1nBOWZ2dmO2aX;uJIF{e2G7 MUixMlIhdU1? M3XzPGROW09? M{DnbolvcGmkaYTzJG1qfG:2aXOgR4xwdmGuIFX4dIFve2mxbh?= NIqzZVMyQTR6M{OwOC=>
3T3-L1 MWLjfZRwfG:6aXPpeJkh[XO|YYm= NEnZSosyNjJibV2= MkPWSG1UVw>? MX;k[YNz\WG|ZYOgR4VtdCCYaXHibYxqfHl? NXLLXWlqOTl2OEOzNFQ>
3T3-L1 MW\LbY5ie2ViYYPzZZk> NFfhR|YyNjJibV2= NGO2fIlFVVOR M4HxT4FkfGm4YYTld{BCVVCN NVfzcm9lOTl2OEOzNFQ>
L6 skeletal muscle cells MUHGeY5kfGmxbjDhd5NigQ>? MmfNNlUxKM7:TR?= NF;aN3dFVVOR NGXHbYhi[3SrdnH0[ZMhSU2SSzDzbYdv[WyrbnegdIF1cHejeYO= NHvOVpgyQTh{OEizOi=>
L6 skeletal muscle cells M4jHOmZ2dmO2aX;uJIF{e2G7 MoLYNlUxKM7:TR?= MVHEUXNQ MXPpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= M2TVW|E6QDJ6OEO2
MDA-MB231 MWjBdI9xfG:|aYOgZZN{[Xl? M17PbFQxOCEQvF2= NVvwS41zTE2VTx?= NVW4ZlRqe2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= M4[0UFE6QDl4NE[5
BT474 MYLBdI9xfG:|aYOgZZN{[Xl? MmXCOFAxKM7:TR?= NVvaVoJVTE2VTx?= MV7z[Y5{cXSrenXzJIh2dWGwIHLy[YF{fCClYX7j[ZIh[2WubDDsbY5meyC2bzDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqew>? MlOxNVk5QTZ2Nkm=
MCF7 MVvBdI9xfG:|aYOgZZN{[Xl? NH3BZow1ODBizszN NXXUOoMyTE2VTx?= NFjSR|l{\W6|aYTpfoV{KGi3bXHuJIJz\WG|dDDjZY5k\XJiY3XscEBtcW6nczD0c{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orcx?= NEny[3kyQTh7NkS2PS=>
Mesenchymal stem cells NV[y[mhRU2mwYYPlJIF{e2G7 NHfGcGsyOCEEtV2= MULEUXNQ NX;UXpVycW6mdXPld{BiKHKxYoXzeEBidmRic4XzeIFqdmWmIFHNVGsh[WO2aY\heIlwdg>? NWrk[GFDOjRzMES4O|k>
Mesenchymal stem cells NIrvcoFkgXSxdH;4bYNqfHliYYPzZZk> MkfXNVAxKML3TR?= Mn7PSG1UVw>? NIPuboll\WO{ZXHz[ZMhfGinIF3TR{Bxem:uaX\ldoF1cW:w MmriNlQyODR6N{m=
MG-63 NV\0XFlo[3m2b4TvfIlkcXS7IHHzd4F6 NFTkPGUyOCEEtV2= NHj2Oo9FVVOR MmqzbY5pcWKrdIOgTFJQOi2LbnT1Z4VlKE:|dHXvZoxie3RiQ3XscEBF\WG2aB?= NHTiSnYzPDl4MEO2Ni=>
MC3T3-E1 M4D5c4N6fG:2b4jpZ4l1gSCjc4PhfS=> NWPWPVh2OTBiwsXN NUPkcVJ6TE2VTx?= NHnBZmhqdmirYnn0d{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKESnYYTo NX60SHpCOjR7NkCzOlI>
MG-63 NV7mdWsxSXCxcITvd4l{KGG|c3H5 Mn7aNVAhyrWP NYPU[IljTE2VTx?= NXzNcoFze3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= NW\leWk{OjR7NkCzOlI>
MC3T3-E1 NE\ETXJCeG:ydH;zbZMh[XO|YYm= MonkNVAhyrWP NY\QZZdHTE2VTx?= NYLCcZl3e3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= NWOzeZRlOjR7NkCzOlI>
MG-63 NWnpdYdlTnWwY4Tpc44h[XO|YYm= NUTWSmh[OTBiwsXN MkTLSG1UVw>? M3j1V4FtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= NFWwcGIzPDl4MEO2Ni=>
MC3T3-E1 NVywS4k{TnWwY4Tpc44h[XO|YYm= NXq5S3BLOTBiwsXN NUDjbpQ5TE2VTx?= M2nwXYFtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= NIXsT4czPDl4MEO2Ni=>
MG-63 MWLGeY5kfGmxbjDhd5NigQ>? NXTJZnRkOTBiwsXN MVfEUXNQ M2rEZYZi[2muaYTheIV{KEh{T{KtbY5lfWOnZDDheZRweGijZ4mgZYN1cX[jdHnvci=> MWqyOFk3ODN4Mh?=
MC3T3-E1 NGTB[IxHfW6ldHnvckBie3OjeR?= NWnCToxXOTBiwsXN NGW2SlFFVVOR NHe3N3Fn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> NVKyd2x[OjR7NkCzOlI>
PC3 M3jDc2tqdmG|ZTDhd5NigQ>? NUTjepd[OTByINM1US=> MWHEUXNQ NHTwXmR2eHKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJGFOWEtiYX7kJGFESyCyaH;zdIhwenmuYYTpc44> NFzCdVkzPTV7NEC0Ny=>
PC3M MlmyT4lv[XOnIHHzd4F6 MmLpNVAxKML3TR?= NEfafINFVVOR MofJeZBz\We3bHH0[ZMhfGinIHzleoVteyCxZjDBUXBMKGGwZDDBR2MheGixc4Doc5J6dGG2aX;u NVr5eFVPOjV3OUSwOFM>
PC3 NXnUWWtvTnWwY4Tpc44h[XO|YYm= MXuxNFAhyrWP MX3EUXNQ MlT3bY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= MYGyOVU6PDB2Mx?=
PC3M MVPGeY5kfGmxbjDhd5NigQ>? MVKxNFAhyrWP M1XiOWROW09? NI\PPYJqdmS3Y3XzJHBKO0txbWTPVkBx[XSqd3H5dy=> M334eFI2PTl2MESz
PC3 NVTTN21TT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUSxNFAhyrWP NHTSR4ZFVVOR M1e2eZN2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbh?= NV7jbm1KOjV3OUSwOFM>
PC3M MkHGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MlOyNVAxKML3TR?= NUnBb41uTE2VTx?= NXq2TlZqe3WycILld5NmeyCycn;sbYZmemG2aX;u Mn7GNlU2QTRyNEO=
MC3T3-E1 NIm0ZndMcW6jc3WgZZN{[Xl? NF7adZgyOCEQvF2= NFLwflNFVVOR NE\QfHpqdmS3Y3XzJJNq\26rZnnjZY51KEGPUFugZYN1cX[jdHnvci=> NX\FVZM1OjZ6OUG4OlY>
MC3T3-E1 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVPxbGEzOTBizszN M1vjd2ROW09? Mn[zbY5pcWKrdIOgSIV5NWmwZIXj[YQhd3O2ZX;icIF{fCClZXzsJIRm[XSq NFrLdnUzPjh7MUi2Oi=>
MC3T3-E1 NYe2WFNITnWwY4Tpc44h[XO|YYm= MVKxNEDPxE1? MUPEUXNQ NYHt[Hg1cW6qaXLpeJMhTGW6LXnu[JVk\WRib4jp[IF1cX[nIIP0doV{ew>? NILFbFczPjh7MUi2Oi=>

... 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]

Protocol

Kinase Assay
+ Expand

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
+ Expand
  • Cell lines: MEF cells
  • Concentrations: 300 μM
  • Incubation Time: 24 hours
  • Method:

    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)
Animal Research
+ Expand
  • Animal Models: Sprague Dawley rats
  • Formulation: A-769662 is dissolved in DMSO.
  • Dosages: 30 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

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

* 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.

Chemical Information

Molecular Weight 360.39
Formula

C20H12N2O3S

CAS No. 844499-71-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID