A-769662

For research use only.

Catalog No.S2697

35 publications

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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Selleck's A-769662 has been cited by 35 publications

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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 M4XWbWZ2dmO2aX;uJIF{e2G7 MX2xJI1O MYfEUXNQ NFrEdopqdmirYnn0d{Bn[XS2eTDhZ4llKHO7boTo[ZNqeyC5aYToJGlEPTBib3[gN{43KM7:TR?= Mlr1NVY4PTN3N{[=
rat hepatocytes M1OycGZ2dmO2aX;uJIF{e2G7 NGrSR5EyKG2P NEnxeJZFVVOR MVnpcohq[mm2czDmZZR1gSCjY3nkJJN6dnSqZYPpd{B4cXSqIFnDOVAhd2ZiMz62JO69VQ>? NF;ORnMyPjd3M{W3Oi=>
HEK293 NV\NeZJDU2mwYYPlJIF{e2G7 MmO3NlAxKM7:TR?= NILCe2NFVVOR MYThZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN NELucYkyPzd{OEK0NS=>
CCL13 M4nONWtqdmG|ZTDhd5NigQ>? NYm4NXZoOjByIN88US=> MWrEUXNQ MWDhZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN MnzCNVc4Ojh{NEG=
MEFs MoXuSpVv[3Srb36gZZN{[Xl? MkeyN|AxKM7:TR?= MoLlSG1UVw>? NXPzSpNDcW6qaXLpeJMheHKxdHXhd49u[WxiZoXuZ5Rqd25iYomgZY4hSU2SSz3pcoRmeGWwZHXueEBu\WOqYX7pd40> MlTONVg2QTN3OES=
epididymal clear cells Ml;SSpVv[3Srb36gZZN{[Xl? MX[yNFAh|ryP NFjVeZFFVVOR MVjpcohq[mm2czD0bIUheEhvbXXkbYF1\WRiVj3BWHBie2ViYXPjeY12dGG2aX;uJIF1KHSqZTDhdIlk[WxibXXtZpJidmV? MmnnNVkzOTF7MUi=
3T3-L1 MU\GeY5kfGmxbjDhd5NigQ>? M1LJ[VEvOiCvTR?= MmrwSG1UVw>? NX3EUphtcW6qaXLpeJMhO1R|LVyxJGFlcXCxZ3Xu[ZNqew>? MonRNVk1QDN|MES=
3T3-L1 M1HrWmZ2dmO2aX;uJIF{e2G7 MnjwNU4zKG2P NYHifFdtTE2VTx?= NHn4b|JqdmirYnn0d{B1cGViRYjwdoV{e2mxbjDv[kBC\Gmyb3flcoV{cXOUZXzheIVlKFS{YX7zZ5JqeHSrb36gSoFkfG:{czDhcoQhVWG{a3Xydy=> NU\i[os6OTl2OEOzNFQ>
3T3-L1 NWfiUZVITnWwY4Tpc44h[XO|YYm= MonVNU4zKG2P NYjxOnppTE2VTx?= MmW5bY5pcWKrdIOgUYl1d3SrYzDDcI9v[WxiRYjwZY5{cW:w M33iflE6PDh|M{C0
3T3-L1 NVq2[ZdM[3m2b4TvfIlkcXS7IHHzd4F6 MoHPNU4zKG2P M{TPTmROW09? NVfrRZdQ\GWlcnXhd4V{KEOnbHygWoli[mmuaYT5 NYrRd4k{OTl2OEOzNFQ>
3T3-L1 MYnLbY5ie2ViYYPzZZk> NIjOSo0yNjJibV2= NYrXWlBITE2VTx?= M{LUNoFkfGm4YYTld{BCVVCN M4HRVlE6PDh|M{C0
L6 skeletal muscle cells M1TjOWZ2dmO2aX;uJIF{e2G7 NWW1Wox{OjVyIN88US=> MWLEUXNQ NFPzV|hi[3SrdnH0[ZMhSU2SSzDzbYdv[WyrbnegdIF1cHejeYO= NYi4XohoOTl6Mki4N|Y>
L6 skeletal muscle cells NFPo[nNHfW6ldHnvckBie3OjeR?= NVPnbZlnOjVyIN88US=> MnzvSG1UVw>? MWLpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= Mor2NVk5Ojh6M{[=
MDA-MB231 M2LXdmFxd3C2b4Ppd{Bie3OjeR?= NUHZcY9NPDByIN88US=> NELzfpRFVVOR M13vd5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MX2xPVg6PjR4OR?=
BT474 MW\BdI9xfG:|aYOgZZN{[Xl? M{TMN|QxOCEQvF2= NVnDPWhZTE2VTx?= NX7UcFlYe2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= NEPmdIEyQTh7NkS2PS=>
MCF7 NWLXd2s3SXCxcITvd4l{KGG|c3H5 NVPqcHpQPDByIN88US=> MVzEUXNQ NWK1OmE5e2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= MkTDNVk5QTZ2Nkm=
Mesenchymal stem cells NYqzUZQxU2mwYYPlJIF{e2G7 M3raOFExKML3TR?= MUPEUXNQ M2i5Nolv\HWlZYOgZUBzd2K3c4SgZY5lKHO3c4ThbY5m\CCDTWDLJIFkfGm4YYTpc44> NECzWFEzPDFyNEi3PS=>
Mesenchymal stem cells M1fPdYN6fG:2b4jpZ4l1gSCjc4PhfS=> MmC0NVAxKML3TR?= NYDDS4RkTE2VTx?= Mn\v[IVkemWjc3XzJJRp\SCPU1OgdJJwdGmoZYLheIlwdg>? NWDXdVI{OjRzMES4O|k>
MG-63 NVryNWM1[3m2b4TvfIlkcXS7IHHzd4F6 NXfTNJdoOTBiwsXN NGnUTotFVVOR MVrpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq NGnvSHMzPDl4MEO2Ni=>
MC3T3-E1 M{XpSYN6fG:2b4jpZ4l1gSCjc4PhfS=> NFPGOWsyOCEEtV2= NGrTOpNFVVOR MVvpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq MYmyOFk3ODN4Mh?=
MG-63 MVTBdI9xfG:|aYOgZZN{[Xl? MmS2NVAhyrWP NGTYbVJFVVOR MlL0d5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? M{L1OVI1QTZyM{[y
MC3T3-E1 MoPSRZBweHSxc3nzJIF{e2G7 MkLhNVAhyrWP NHXZb|VFVVOR MkDMd5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? NI\TN|MzPDl4MEO2Ni=>
MG-63 NFHKXoVHfW6ldHnvckBie3OjeR?= MYixNEDDvU1? NUmyO3pUTE2VTx?= NIjXOoNidGyndnnheIV{KFKRUzDhZ4N2dXWuYYTpc44h[W6mIFHUVEBl\XCuZYTpc44h[2G3c3XkJIJ6KEh{T{K= NIS3T2ozPDl4MEO2Ni=>
MC3T3-E1 NVPDZ|hnTnWwY4Tpc44h[XO|YYm= NV7ZNo86OTBiwsXN MV7EUXNQ MnfTZYxt\X[rYYTld{BTV1NiYXPjeY12dGG2aX;uJIFv\CCDVGCg[IVxdGW2aX;uJINifXOnZDDifUBJOk9{ Mk\kNlQ6PjB|NkK=
MG-63 NFPFWGZHfW6ldHnvckBie3OjeR?= MojTNVAhyrWP MmDtSG1UVw>? NG\6Zlhn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> M4T4NlI1QTZyM{[y
MC3T3-E1 MYHGeY5kfGmxbjDhd5NigQ>? MWKxNEDDvU1? M1fKRWROW09? NWXjW3FO\mGlaXzpeIF1\XNiSELPNk1qdmS3Y3XkJIF2fG:yaHHnfUBi[3SrdnH0bY9v MWqyOFk3ODN4Mh?=
PC3 M2nWZWtqdmG|ZTDhd5NigQ>? MWqxNFAhyrWP NVPGOXRHTE2VTx?= NU[xZlNyfXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v NXr3TZhHOjV3OUSwOFM>
PC3M NHrpUVBMcW6jc3WgZZN{[Xl? NXPo[21HOTByINM1US=> MoP5SG1UVw>? M2rBd5VxemWpdXzheIV{KHSqZTDs[ZZmdHNib3[gRW1RUyCjbnSgRWNEKHCqb4PwbI9zgWyjdHnvci=> NGn6VHgzPTV7NEC0Ny=>
PC3 MUHGeY5kfGmxbjDhd5NigQ>? NHvLUo0yODBiwsXN MlLFSG1UVw>? NYXmVnVucW6mdXPld{BRUTONL33UU3IheGG2aIfhfZM> M36wclI2PTl2MESz
PC3M MVfGeY5kfGmxbjDhd5NigQ>? MmHrNVAxKML3TR?= MkmxSG1UVw>? MlrEbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= NGPzRYszPTV7NEC0Ny=>
PC3 MmjiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MnnkNVAxKML3TR?= MVPEUXNQ Ml7pd5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:w NVW5WXVMOjV3OUSwOFM>
PC3M NGTrZ4dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlzaNVAxKML3TR?= NX3zXWIzTE2VTx?= MYrzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? Mlf5NlU2QTRyNEO=
MC3T3-E1 NGHINHRMcW6jc3WgZZN{[Xl? M4nBbFExKM7:TR?= MUnEUXNQ NV;LboRZcW6mdXPld{B{cWewaX\pZ4FvfCCDTWDLJIFkfGm4YYTpc44> MY[yOlg6OTh4Nh?=
MC3T3-E1 MljzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NYPjeIVCOTBizszN MXvEUXNQ NVjkNJZYcW6qaXLpeJMhTGW6LXnu[JVk\WRib4P0[Y9jdGG|dDDj[YxtKGSnYYTo NGXOXIYzPjh7MUi2Oi=>
MC3T3-E1 MUDGeY5kfGmxbjDhd5NigQ>? NU\zeFR1OTBizszN M3vPc2ROW09? MWfpcohq[mm2czDE[ZgucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz M{HvO|I3QDlzOE[2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pCofilin / Cofilin / detyrosinated alpha tubulin / acetylated alpha tubulin ; 

PubMed: 26431377     


A & B. MCF-7 cells were treated with 100–400 μM of A-769662 for 4-24 hours. Protein was harvested and Western blot analysis was done to determine levels of pAMPK at threonine 172, pCofilin at serine 3, detyrosinated alpha tubulin (glu-tub), and acetylated alpha tubulin (acetyl-tub). C & D. BT-549 cells were treated with 100–400 μM A-769662 for 4–24 hours. Protein was harvested and Western blot analysis was done to determine levels of markers listed above.

p-AMPK / AMPK / p-S6K / S6K / p-ACC ; 

PubMed: 22456226     


Representative immunoblots for p-AMPK, total AMPK, p-S6K, total S6K, p-ACC and actin under control conditions (C) and in response to 50 μM A-769662 at various time points.

26431377 22456226
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]

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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]

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  • 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]

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  • Animal Models: Sprague Dawley rats
  • 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):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.
5 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
Smiles OC1=CC=CC=C1C2=CC=C(C=C2)C3=CSC4=C3C(=C(C#N)C(=O)N4)O

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AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID