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.

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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.

    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.

  • 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.

    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

Choose Selective AMPK Inhibitors

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]
(in primary rat hepatocytes)
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 M1rqd2Z2dmO2aX;uJIF{e2G7 MlLrNUBuVQ>? NWnJSVI4TE2VTx?= MmXQbY5pcWKrdIOg[oF1fHliYXPp[EB{gW62aHXzbZMhf2m2aDDJR|UxKG:oIEOuOkDPxE1? NXvYcoFlOTZ5NUO1O|Y>
rat hepatocytes M2Xi[WZ2dmO2aX;uJIF{e2G7 M2TOVFEhdU1? MW\EUXNQ MXPpcohq[mm2czDmZZR1gSCjY3nkJJN6dnSqZYPpd{B4cXSqIFnDOVAhd2ZiMz62JO69VQ>? M1PRZlE3PzV|NUe2
HEK293 NVvzVmpsU2mwYYPlJIF{e2G7 MnKyNlAxKM7:TR?= NIrzeYxFVVOR NEC2SJBi[3SrdnH0[ZMh\W6mb3flco92eyCDTWDL NIjPS|YyPzd{OEK0NS=>
CCL13 NE\HeVVMcW6jc3WgZZN{[Xl? NVrSNlAzOjByIN88US=> NI\afpFFVVOR MmjMZYN1cX[jdHXzJIVv\G:pZX7veZMhSU2SSx?= NX\HOmp6OTd5MkiyOFE>
MEFs MUXGeY5kfGmxbjDhd5NigQ>? MVuzNFAh|ryP M1vKOmROW09? MnzQbY5pcWKrdIOgdJJwfGWjc3;tZYwh\nWwY4Tpc44h[nliYX6gRW1RUy2rbnTldIVv\GWwdDDt[YNp[W6rc32= M1TjcVE5PTl|NUi0
epididymal clear cells NFG3NYZHfW6ldHnvckBie3OjeR?= NIXJUGUzODBizszN NE[xW5VFVVOR NFXSe3ZqdmirYnn0d{B1cGVicFitcYVlcWG2ZXSgWk1CXFCjc3WgZYNkfW23bHH0bY9vKGG2IITo[UBieGmlYXygcYVu[nKjbnW= NGLFXnEyQTJzMUmxPC=>
3T3-L1 MoLDSpVv[3Srb36gZZN{[Xl? MXGxMlIhdU1? NHnFdXpFVVOR NIXpNolqdmirYnn0d{A{XDNvTEGgRYRqeG:pZX7ld4l{ NYLOcIZXOTl2OEOzNFQ>
3T3-L1 M{X1WmZ2dmO2aX;uJIF{e2G7 M4\OU|EvOiCvTR?= M3;oVmROW09? MXfpcohq[mm2czD0bIUhTXiycnXzd4lwdiCxZjDB[Ilxd2enbnXzbZNT\WyjdHXkJHRz[W6|Y4LpdJRqd25iRnHjeI9zeyCjbnSgUYFzc2W{cx?= NULQd4UxOTl2OEOzNFQ>
3T3-L1 MonuSpVv[3Srb36gZZN{[Xl? M1fRc|EvOiCvTR?= NWnId|NmTE2VTx?= MVPpcohq[mm2czDNbZRwfGmlIFPsc45idCCHeIDhcpNqd25? MnrmNVk1QDN|MES=
3T3-L1 NXjROVJt[3m2b4TvfIlkcXS7IHHzd4F6 MnGzNU4zKG2P MYPEUXNQ MUHk[YNz\WG|ZYOgR4VtdCCYaXHibYxqfHl? NH;6[JIyQTR6M{OwOC=>
3T3-L1 NH60dm9McW6jc3WgZZN{[Xl? NEHkVlcyNjJibV2= NU[1SpJOTE2VTx?= MmjaZYN1cX[jdHXzJGFOWEt? NIHjNpoyQTR6M{OwOC=>
L6 skeletal muscle cells NUPIcFdlTnWwY4Tpc44h[XO|YYm= NGnrNmMzPTBizszN MmG4SG1UVw>? MW\hZ5RqfmG2ZYOgRW1RUyC|aXfuZYxqdmdicHH0bJdigXN? NH7rTnQyQTh{OEizOi=>
L6 skeletal muscle cells NFP6VnpHfW6ldHnvckBie3OjeR?= MYmyOVAh|ryP MX;EUXNQ MX\pcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= MXixPVgzQDh|Nh?=
MDA-MB231 MoD6RZBweHSxc3nzJIF{e2G7 M2TlXFQxOCEQvF2= Mn63SG1UVw>? M{XvXJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M1fWflE6QDl4NE[5
BT474 NFflbYxCeG:ydH;zbZMh[XO|YYm= Mnv4OFAxKM7:TR?= MXTEUXNQ MlXmd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? NF;abXIyQTh7NkS2PS=>
MCF7 MYfBdI9xfG:|aYOgZZN{[Xl? MlezOFAxKM7:TR?= M1LBbWROW09? MYPz[Y5{cXSrenXzJIh2dWGwIHLy[YF{fCClYX7j[ZIh[2WubDDsbY5meyC2bzDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqew>? MoW1NVk5QTZ2Nkm=
Mesenchymal stem cells M4CxWWtqdmG|ZTDhd5NigQ>? NETrRmYyOCEEtV2= MknrSG1UVw>? MVHpcoR2[2W|IHGgdo9jfXO2IHHu[EB{fXO2YXnu[YQhSU2SSzDhZ5RqfmG2aX;u MViyOFExPDh5OR?=
Mesenchymal stem cells NFPhPZFkgXSxdH;4bYNqfHliYYPzZZk> NXzTOJp6OTByINM1US=> NHj2cIFFVVOR NV7lWmxD\GWlcnXhd4V{KHSqZTDNV2MheHKxbHnm[ZJifGmxbh?= MkDnNlQyODR6N{m=
MG-63 M3z1XoN6fG:2b4jpZ4l1gSCjc4PhfS=> MnHlNVAhyrWP NEXDSJNFVVOR Mlj3bY5pcWKrdIOgTFJQOi2LbnT1Z4VlKE:|dHXvZoxie3RiQ3XscEBF\WG2aB?= NGe0TFkzPDl4MEO2Ni=>
MC3T3-E1 MljUZ5l1d3SxeHnjbZR6KGG|c3H5 NHT3cJAyOCEEtV2= NGm2d4dFVVOR NYjOcllMcW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> NGnhR4czPDl4MEO2Ni=>
MG-63 NF;ENm9CeG:ydH;zbZMh[XO|YYm= M2Hn[FExKML3TR?= MXHEUXNQ NUG3VI8xe3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= NIHNcm0zPDl4MEO2Ni=>
MC3T3-E1 NFXUUoZCeG:ydH;zbZMh[XO|YYm= NXT6[2loOTBiwsXN NHvPVWFFVVOR Mn7ud5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? M37qRlI1QTZyM{[y
MG-63 NV33WopwTnWwY4Tpc44h[XO|YYm= NILIT2EyOCEEtV2= MmjZSG1UVw>? NFfoVmpidGyndnnheIV{KFKRUzDhZ4N2dXWuYYTpc44h[W6mIFHUVEBl\XCuZYTpc44h[2G3c3XkJIJ6KEh{T{K= NVP5UHk5OjR7NkCzOlI>
MC3T3-E1 NV\DRosyTnWwY4Tpc44h[XO|YYm= MkK4NVAhyrWP M4H3e2ROW09? MXrhcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? MnPLNlQ6PjB|NkK=
MG-63 NHPybIhHfW6ldHnvckBie3OjeR?= NWrxXmxKOTBiwsXN NXi4T4JsTE2VTx?= NFnCdXhn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> MUmyOFk3ODN4Mh?=
MC3T3-E1 NH7aNlZHfW6ldHnvckBie3OjeR?= M3fXb|ExKML3TR?= MU\EUXNQ Ml7D[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u MX[yOFk3ODN4Mh?=
PC3 MlrUT4lv[XOnIHHzd4F6 NFu2R|gyODBiwsXN MkPmSG1UVw>? M3vSXJVxemWpdXzheIV{KHSqZTDs[ZZmdHNib3[gRW1RUyCjbnSgRWNEKHCqb4PwbI9zgWyjdHnvci=> MoLjNlU2QTRyNEO=
PC3M MV7LbY5ie2ViYYPzZZk> MYCxNFAhyrWP NIrnRlBFVVOR NU\1NIFGfXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v MmLoNlU2QTRyNEO=
PC3 NYL4XXRVTnWwY4Tpc44h[XO|YYm= MlHmNVAxKML3TR?= MX\EUXNQ MmDibY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= M2ntNlI2PTl2MESz
PC3M NHXEdldHfW6ldHnvckBie3OjeR?= MVmxNFAhyrWP M3rIS2ROW09? M1fOVYlv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz MUKyOVU6PDB2Mx?=
PC3 M4rQemdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NE[xNpAyODBiwsXN M1P6S2ROW09? Mlnyd5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:w MkjnNlU2QTRyNEO=
PC3M NXv0SJBTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MUSxNFAhyrWP M2\wc2ROW09? M3OyfZN2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbh?= MX:yOVU6PDB2Mx?=
MC3T3-E1 NYW1fI16U2mwYYPlJIF{e2G7 NHLDW3UyOCEQvF2= NYjoW|VvTE2VTx?= NIP2fnNqdmS3Y3XzJJNq\26rZnnjZY51KEGPUFugZYN1cX[jdHnvci=> MnPRNlY5QTF6Nk[=
MC3T3-E1 NWqzTZc2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmnHNVAh|ryP MnGySG1UVw>? NVzPR4FOcW6qaXLpeJMhTGW6LXnu[JVk\WRib4P0[Y9jdGG|dDDj[YxtKGSnYYTo M2nOWFI3QDlzOE[2
MC3T3-E1 NF3aOnZHfW6ldHnvckBie3OjeR?= Mnn3NVAh|ryP NWfnTGI1TE2VTx?= NGPzd2NqdmirYnn0d{BF\XhvaX7keYNm\CCxeHnkZZRqfmVic4Ty[ZN{ MlToNlY5QTF6Nk[=

... 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:

[1]
+ 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:

[3]
+ 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:

[1]
+ 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing. 		30 mg/mL

* 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID