A-769662

For research use only.

Catalog No.S2697

37 publications

A-769662 Chemical Structure

CAS No. 844499-71-4

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 37 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 M1jyUWZ2dmO2aX;uJIF{e2G7 MoDzNUBuVQ>? NV;SUGRuTE2VTx?= NVjRT4pNcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= NWfOdpplOTZ5NUO1O|Y>
rat hepatocytes NF2zPWpHfW6ldHnvckBie3OjeR?= MUGxJI1O NYL0eZh6TE2VTx?= M364bIlvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP MXWxOlc2OzV5Nh?=
HEK293 Mkn3T4lv[XOnIHHzd4F6 M4LEXFIxOCEQvF2= NUW4TlZoTE2VTx?= NU\VR5Bw[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> Mn;rNVc4Ojh{NEG=
CCL13 NXvJ[HhOU2mwYYPlJIF{e2G7 NES4NZQzODBizszN M2P2ZWROW09? NXjTendo[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> MXWxO|czQDJ2MR?=
MEFs NYnFOZpTTnWwY4Tpc44h[XO|YYm= MlSxN|AxKM7:TR?= M4e0SGROW09? MkjTbY5pcWKrdIOgdJJwfGWjc3;tZYwh\nWwY4Tpc44h[nliYX6gRW1RUy2rbnTldIVv\GWwdDDt[YNp[W6rc32= NVnY[Hk5OTh3OUO1PFQ>
epididymal clear cells NUf2cFBlTnWwY4Tpc44h[XO|YYm= NW\0UXA5OjByIN88US=> NEnuOlZFVVOR M4DVfYlvcGmkaYTzJJRp\SCySD3t[YRq[XSnZDDWMWFVWGG|ZTDhZ4N2dXWuYYTpc44h[XRidHjlJIFxcWOjbDDt[Y1jemGwZR?= MWmxPVIyOTlzOB?=
3T3-L1 NUm0b4Z2TnWwY4Tpc44h[XO|YYm= NWTYeVd4OS5{IH3N Ml;oSG1UVw>? MYTpcohq[mm2czCzWFMuVDFiQXTpdI9o\W6nc3nz M4DrdFE6PDh|M{C0
3T3-L1 MYnGeY5kfGmxbjDhd5NigQ>? MWOxMlIhdU1? NHzMc4FFVVOR M1\wc4lvcGmkaYTzJJRp\SCHeIDy[ZN{cW:wIH;mJGFlcXCxZ3Xu[ZNqe1KnbHH0[YQhXHKjboPjdolxfGmxbjDGZYN1d3K|IHHu[EBO[XKtZYLz MUixPVQ5OzNyNB?=
3T3-L1 MmnzSpVv[3Srb36gZZN{[Xl? Ml3tNU4zKG2P MWXEUXNQ NWPsO|ZicW6qaXLpeJMhVWm2b4TpZ{BEdG:wYXygSZhx[W6|aX;u NEjnemgyQTR6M{OwOC=>
3T3-L1 MmP0Z5l1d3SxeHnjbZR6KGG|c3H5 MWCxMlIhdU1? MUDEUXNQ NVrRR4tm\GWlcnXhd4V{KEOnbHygWoli[mmuaYT5 M2HFeVE6PDh|M{C0
3T3-L1 MXrLbY5ie2ViYYPzZZk> M{LkT|EvOiCvTR?= MWLEUXNQ MYjhZ5RqfmG2ZYOgRW1RUw>? NIjsXpUyQTR6M{OwOC=>
L6 skeletal muscle cells M1;OfWZ2dmO2aX;uJIF{e2G7 MXSyOVAh|ryP MWTEUXNQ NVW5WIhI[WO2aY\heIV{KEGPUFugd4lodmGuaX7nJJBifGi5YYnz M1jtd|E6QDJ6OEO2
L6 skeletal muscle cells Ml3YSpVv[3Srb36gZZN{[Xl? MVeyOVAh|ryP M3i4bWROW09? MYnpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= M4DoblE6QDJ6OEO2
MDA-MB231 M{LUOWFxd3C2b4Ppd{Bie3OjeR?= NX\NR29[PDByIN88US=> MmfTSG1UVw>? M2j2epNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| M3rmfFE6QDl4NE[5
BT474 M{Ttb2Fxd3C2b4Ppd{Bie3OjeR?= NEHwdmw1ODBizszN MVXEUXNQ MoT1d4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? NGjEdmoyQTh7NkS2PS=>
MCF7 Mm\iRZBweHSxc3nzJIF{e2G7 MXy0NFAh|ryP NUTEd3F7TE2VTx?= MYPz[Y5{cXSrenXzJIh2dWGwIHLy[YF{fCClYX7j[ZIh[2WubDDsbY5meyC2bzDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqew>? MUmxPVg6PjR4OR?=
Mesenchymal stem cells NYHXRpR2U2mwYYPlJIF{e2G7 MUOxNEDDvU1? NXrQelRGTE2VTx?= MoLHbY5lfWOnczDhJJJw[nW|dDDhcoQhe3W|dHHpcoVlKEGPUFugZYN1cX[jdHnvci=> MoLPNlQyODR6N{m=
Mesenchymal stem cells M2TUfYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYWxNFAhyrWP NUXTXHM4TE2VTx?= NUjhSHdE\GWlcnXhd4V{KHSqZTDNV2MheHKxbHnm[ZJifGmxbh?= NVzPeI5bOjRzMES4O|k>
MG-63 MkXGZ5l1d3SxeHnjbZR6KGG|c3H5 MX2xNEDDvU1? NEfUWllFVVOR NHvR[W9qdmirYnn0d{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKESnYYTo NEfhUmEzPDl4MEO2Ni=>
MC3T3-E1 MV7jfZRwfG:6aXPpeJkh[XO|YYm= NFK2[5cyOCEEtV2= NGL1XHVFVVOR MVLpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq NE\nU5ozPDl4MEO2Ni=>
MG-63 MX;BdI9xfG:|aYOgZZN{[Xl? NW\6dWJWOTBiwsXN NFLSWXpFVVOR Mnfpd5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? M4XPdFI1QTZyM{[y
MC3T3-E1 MlfpRZBweHSxc3nzJIF{e2G7 Mnz3NVAhyrWP NX7HcYV7TE2VTx?= MojKd5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? MXuyOFk3ODN4Mh?=
MG-63 MoHWSpVv[3Srb36gZZN{[Xl? MoDNNVAhyrWP Ml7GSG1UVw>? MVPhcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? M4fVWFI1QTZyM{[y
MC3T3-E1 M1LNZWZ2dmO2aX;uJIF{e2G7 MoWyNVAhyrWP MUPEUXNQ M4jCPYFtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= MUSyOFk3ODN4Mh?=
MG-63 Mn3ZSpVv[3Srb36gZZN{[Xl? Mn\ZNVAhyrWP NWXiVoJkTE2VTx?= MUfmZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36= NHzHeIszPDl4MEO2Ni=>
MC3T3-E1 NIXtRZVHfW6ldHnvckBie3OjeR?= NHW1bWMyOCEEtV2= NYnjPFBnTE2VTx?= Mmro[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NGDJWGEzPDl4MEO2Ni=>
PC3 MWTLbY5ie2ViYYPzZZk> MknQNVAxKML3TR?= MW\EUXNQ MmfCeZBz\We3bHH0[ZMhfGinIHzleoVteyCxZjDBUXBMKGGwZDDBR2MheGixc4Doc5J6dGG2aX;u NHXTWIIzPTV7NEC0Ny=>
PC3M MkPXT4lv[XOnIHHzd4F6 M2rFWFExOCEEtV2= MnjNSG1UVw>? NYjycVdPfXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v MlfVNlU2QTRyNEO=
PC3 MmrjSpVv[3Srb36gZZN{[Xl? Mnq2NVAxKML3TR?= MVnEUXNQ M3LXT4lv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz NVvhVWk1OjV3OUSwOFM>
PC3M NIT2[|dHfW6ldHnvckBie3OjeR?= M2T6eFExOCEEtV2= MU\EUXNQ M3PhT4lv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz NF3EcGgzPTV7NEC0Ny=>
PC3 NGrpb3dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2[zWFExOCEEtV2= MWfEUXNQ NWLVR3doe3WycILld5NmeyCycn;sbYZmemG2aX;u M3LWWVI2PTl2MESz
PC3M MX\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXixNFAhyrWP MnX1SG1UVw>? NGLCdWp{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36= NUDuV|AyOjV3OUSwOFM>
MC3T3-E1 M{jHXGtqdmG|ZTDhd5NigQ>? NH\kZlEyOCEQvF2= MX3EUXNQ Mlv3bY5lfWOnczDzbYdvcW[rY3HueEBCVVCNIHHjeIl3[XSrb36= NYO2RnQ2OjZ6OUG4OlY>
MC3T3-E1 M1;lVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGe1R4wyOCEQvF2= MlnzSG1UVw>? NFHmToVqdmirYnn0d{BF\XhvaX7keYNm\CCxc4Tlc4Jt[XO2IHPlcIwh\GWjdHi= M13CS|I3QDlzOE[2
MC3T3-E1 M1ToTGZ2dmO2aX;uJIF{e2G7 MVixNEDPxE1? NVPzSoxuTE2VTx?= M1T5bIlvcGmkaYTzJGRmgC2rbnT1Z4VlKG:6aXTheIl3\SC|dILld5M> NFPnOnAzPjh7MUi2Oi=>

... 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 C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID