A-769662

For research use only. Not for use in humans.

Catalog No.S2697

28 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 28 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 NVnEeYdHTnWwY4Tpc44h[XO|YYm= MljVNUBuVQ>? MYfEUXNQ NILBbHBqdmirYnn0d{Bn[XS2eTDhZ4llKHO7boTo[ZNqeyC5aYToJGlEPTBib3[gN{43KM7:TR?= MYSxOlc2OzV5Nh?=
rat hepatocytes M4\JU2Z2dmO2aX;uJIF{e2G7 M1\nTFEhdU1? MnPCSG1UVw>? NUn2cnZrcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= MoHCNVY4PTN3N{[=
HEK293 MX7LbY5ie2ViYYPzZZk> NVjQZ4dTOjByIN88US=> Mn3OSG1UVw>? M4[0S4FkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= M4LydlE4PzJ6MkSx
CCL13 MnvkT4lv[XOnIHHzd4F6 MoPSNlAxKM7:TR?= MY\EUXNQ M3n6UYFkfGm4YYTld{BmdmSxZ3Xuc5V{KEGPUFu= NFPNbpYyPzd{OEK0NS=>
MEFs NWj1RpVITnWwY4Tpc44h[XO|YYm= NIO4dW8{ODBizszN M4HJb2ROW09? NUn4dox[cW6qaXLpeJMheHKxdHXhd49u[WxiZoXuZ5Rqd25iYomgZY4hSU2SSz3pcoRmeGWwZHXueEBu\WOqYX7pd40> NVHyUlhKOTh3OUO1PFQ>
epididymal clear cells Mn71SpVv[3Srb36gZZN{[Xl? M4LpXVIxOCEQvF2= MYnEUXNQ NYTCWppLcW6qaXLpeJMhfGinIIDIMY1m\GmjdHXkJHYuSVSSYYPlJIFk[3WvdXzheIlwdiCjdDD0bIUh[XCrY3HsJI1mdWK{YX7l MYqxPVIyOTlzOB?=
3T3-L1 MnHTSpVv[3Srb36gZZN{[Xl? NYnIeVM4OS5{IH3N M{\rfGROW09? MnHSbY5pcWKrdIOgN3Q{NUxzIFHkbZBw\2WwZYPpdy=> MWWxPVQ5OzNyNB?=
3T3-L1 M{fTPWZ2dmO2aX;uJIF{e2G7 MW[xMlIhdU1? MVLEUXNQ M{j0cIlvcGmkaYTzJJRp\SCHeIDy[ZN{cW:wIH;mJGFlcXCxZ3Xu[ZNqe1KnbHH0[YQhXHKjboPjdolxfGmxbjDGZYN1d3K|IHHu[EBO[XKtZYLz MUexPVQ5OzNyNB?=
3T3-L1 M3[y[2Z2dmO2aX;uJIF{e2G7 M16yN|EvOiCvTR?= NHnPNVNFVVOR NIfEW|VqdmirYnn0d{BOcXSxdHnjJGNtd26jbDDFfJBidnOrb36= NXTLbW9JOTl2OEOzNFQ>
3T3-L1 NYm1cXZb[3m2b4TvfIlkcXS7IHHzd4F6 NXvi[XQ2OS5{IH3N MWjEUXNQ NEfzfXZl\WO{ZXHz[ZMhS2WubDDWbYFjcWyrdIm= NVGxOVNkOTl2OEOzNFQ>
3T3-L1 MljUT4lv[XOnIHHzd4F6 MV:xMlIhdU1? MUnEUXNQ NWjCcG9K[WO2aY\heIV{KEGPUFu= Ml;WNVk1QDN|MES=
L6 skeletal muscle cells NVrBTWVCTnWwY4Tpc44h[XO|YYm= MYSyOVAh|ryP MUjEUXNQ MorRZYN1cX[jdHXzJGFOWEtic3nncoFtcW6pIIDheIh4[Xm| M2[4NFE6QDJ6OEO2
L6 skeletal muscle cells MlXzSpVv[3Srb36gZZN{[Xl? NFHsTHgzPTBizszN MYPEUXNQ MV7pcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= MU[xPVgzQDh|Nh?=
MDA-MB231 M{Hxb2Fxd3C2b4Ppd{Bie3OjeR?= NIPRUHA1ODBizszN NHnsSJNFVVOR MkTNd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? Ml75NVk5QTZ2Nkm=
BT474 NWfpfm9rSXCxcITvd4l{KGG|c3H5 MmP1OFAxKM7:TR?= MX3EUXNQ M1flOJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M{XNNFE6QDl4NE[5
MCF7 MVvBdI9xfG:|aYOgZZN{[Xl? Mn3COFAxKM7:TR?= NYHYe|lWTE2VTx?= M1\MOJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| Mmr5NVk5QTZ2Nkm=
Mesenchymal stem cells NFzSVpVMcW6jc3WgZZN{[Xl? MkHQNVAhyrWP NGHpVFZFVVOR MW\pcoR2[2W|IHGgdo9jfXO2IHHu[EB{fXO2YXnu[YQhSU2SSzDhZ5RqfmG2aX;u MV:yOFExPDh5OR?=
Mesenchymal stem cells NECwd|ZkgXSxdH;4bYNqfHliYYPzZZk> M4nqTlExOCEEtV2= M4jxbmROW09? MXXk[YNz\WG|ZYOgeIhmKE2VQzDwdo9tcW[ncnH0bY9v M{jNSlI1OTB2OEe5
MG-63 M{HwToN6fG:2b4jpZ4l1gSCjc4PhfS=> M2f2S|ExKML3TR?= NVvRPY05TE2VTx?= MVvpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq NWXSV|NUOjR7NkCzOlI>
MC3T3-E1 MXLjfZRwfG:6aXPpeJkh[XO|YYm= M1LTbFExKML3TR?= NHXyWm5FVVOR NVuwNVdGcW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> M{CzTFI1QTZyM{[y
MG-63 M17LOGFxd3C2b4Ppd{Bie3OjeR?= MYCxNEDDvU1? MmLySG1UVw>? M36xUZN2eHC{ZYPz[ZMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCDcH;weI9{cXN? MViyOFk3ODN4Mh?=
MC3T3-E1 NY\0RYpqSXCxcITvd4l{KGG|c3H5 MV:xNEDDvU1? NEnuVJlFVVOR MXzzeZBxemW|c3XzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhSXCxcITvd4l{ MlTjNlQ6PjB|NkK=
MG-63 MVnGeY5kfGmxbjDhd5NigQ>? NYfKVnhDOTBiwsXN M{H2SGROW09? M{iwN4FtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= MVKyOFk3ODN4Mh?=
MC3T3-E1 NV:5RnpPTnWwY4Tpc44h[XO|YYm= M2jLW|ExKML3TR?= NXvydpR4TE2VTx?= NIr1U2FidGyndnnheIV{KFKRUzDhZ4N2dXWuYYTpc44h[W6mIFHUVEBl\XCuZYTpc44h[2G3c3XkJIJ6KEh{T{K= MXSyOFk3ODN4Mh?=
MG-63 MnTlSpVv[3Srb36gZZN{[Xl? NXHVUGhFOTBiwsXN NFrPR4lFVVOR M4DGd4Zi[2muaYTheIV{KEh{T{KtbY5lfWOnZDDheZRweGijZ4mgZYN1cX[jdHnvci=> NXfE[FBZOjR7NkCzOlI>
MC3T3-E1 Mn\uSpVv[3Srb36gZZN{[Xl? MYmxNEDDvU1? M2TqOGROW09? MlLm[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NHzOUoUzPDl4MEO2Ni=>
PC3 MYnLbY5ie2ViYYPzZZk> MmqxNVAxKML3TR?= M4DI[WROW09? MVT1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= M1ntfVI2PTl2MESz
PC3M M{DDO2tqdmG|ZTDhd5NigQ>? MX[xNFAhyrWP NIPGT4JFVVOR M2LJdZVxemWpdXzheIV{KHSqZTDs[ZZmdHNib3[gRW1RUyCjbnSgRWNEKHCqb4PwbI9zgWyjdHnvci=> NEntUmkzPTV7NEC0Ny=>
PC3 MVvGeY5kfGmxbjDhd5NigQ>? M{\GelExOCEEtV2= MWrEUXNQ NF;uU4ZqdmS3Y3XzJHBKO0txbWTPVkBx[XSqd3H5dy=> MX:yOVU6PDB2Mx?=
PC3M NEPlU2hHfW6ldHnvckBie3OjeR?= M{\OcVExOCEEtV2= MX;EUXNQ MmrobY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= M1z5eVI2PTl2MESz
PC3 MofqS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV;Y[mRmOTByINM1US=> NUXNV|h6TE2VTx?= NWmxUIZme3WycILld5NmeyCycn;sbYZmemG2aX;u M32wV|I2PTl2MESz
PC3M MnfYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MX:xNFAhyrWP MX\EUXNQ NEW0VGJ{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36= NYO4XoxJOjV3OUSwOFM>
MC3T3-E1 M2XhOWtqdmG|ZTDhd5NigQ>? NUH0SZNMOTBizszN MlfJSG1UVw>? M{Do[Ylv\HWlZYOgd4lodmmoaXPhcpQhSU2SSzDhZ5RqfmG2aX;u NYLRXpRYOjZ6OUG4OlY>
MC3T3-E1 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NUjqPG1wOTBizszN M1jzZWROW09? NXTqVXk1cW6qaXLpeJMhTGW6LXnu[JVk\WRib4P0[Y9jdGG|dDDj[YxtKGSnYYTo M2XnU|I3QDlzOE[2
MC3T3-E1 M4O3NWZ2dmO2aX;uJIF{e2G7 NYLtVphCOTBizszN NF3mWZpFVVOR NUDNb|NVcW6qaXLpeJMhTGW6LXnu[JVk\WRib4jp[IF1cX[nIIP0doV{ew>? MUCyOlg6OTh4Nh?=

... 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
  • 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):
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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID