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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Cited by 13 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.

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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 NYLNfpRyTnWwY4Tpc44h[XO|YYm= Mn3jNUBuVQ>? M{XOcWROW09? NX3zV41PcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= MYSxOlc2OzV5Nh?=
rat hepatocytes MWnGeY5kfGmxbjDhd5NigQ>? Ml7vNUBuVQ>? MlPKSG1UVw>? M1zEVYlvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP MVexOlc2OzV5Nh?=
HEK293 NVz5ZmoxU2mwYYPlJIF{e2G7 MnHkNlAxKM7:TR?= M4DNVGROW09? NXzxd5pT[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> NIi2OYcyPzd{OEK0NS=>
CCL13 NHyxZ41McW6jc3WgZZN{[Xl? MVSyNFAh|ryP NYT0cIg3TE2VTx?= MoXOZYN1cX[jdHXzJIVv\G:pZX7veZMhSU2SSx?= NW\vfFZlOTd5MkiyOFE>
MEFs M3PycWZ2dmO2aX;uJIF{e2G7 MWqzNFAh|ryP MkHwSG1UVw>? MmjqbY5pcWKrdIOgdJJwfGWjc3;tZYwh\nWwY4Tpc44h[nliYX6gRW1RUy2rbnTldIVv\GWwdDDt[YNp[W6rc32= Mm\4NVg2QTN3OES=
epididymal clear cells NVPie2lmTnWwY4Tpc44h[XO|YYm= NWS4[pdFOjByIN88US=> MWLEUXNQ NEPsVZRqdmirYnn0d{B1cGVicFitcYVlcWG2ZXSgWk1CXFCjc3WgZYNkfW23bHH0bY9vKGG2IITo[UBieGmlYXygcYVu[nKjbnW= M1HiOVE6OjFzOUG4
3T3-L1 NGTSWmVHfW6ldHnvckBie3OjeR?= MnfCNU4zKG2P MnHvSG1UVw>? NYX1XYl4cW6qaXLpeJMhO1R|LVyxJGFlcXCxZ3Xu[ZNqew>? MV:xPVQ5OzNyNB?=
3T3-L1 MVjGeY5kfGmxbjDhd5NigQ>? MkfpNU4zKG2P M1HZNWROW09? M4rOWYlvcGmkaYTzJJRp\SCHeIDy[ZN{cW:wIH;mJGFlcXCxZ3Xu[ZNqe1KnbHH0[YQhXHKjboPjdolxfGmxbjDGZYN1d3K|IHHu[EBO[XKtZYLz M4G0bFE6PDh|M{C0
3T3-L1 MYDGeY5kfGmxbjDhd5NigQ>? NUm5UmFEOS5{IH3N NGH5NFlFVVOR NUX3b|Q5cW6qaXLpeJMhVWm2b4TpZ{BEdG:wYXygSZhx[W6|aX;u MXOxPVQ5OzNyNB?=
3T3-L1 M{nkNoN6fG:2b4jpZ4l1gSCjc4PhfS=> MYGxMlIhdU1? NH\iRo9FVVOR NGXkVY9l\WO{ZXHz[ZMhS2WubDDWbYFjcWyrdIm= M1fncVE6PDh|M{C0
3T3-L1 MmWyT4lv[XOnIHHzd4F6 NXLVeoNTOS5{IH3N NEnDeJJFVVOR NUW3WmVj[WO2aY\heIV{KEGPUFu= MUSxPVQ5OzNyNB?=
L6 skeletal muscle cells Mn7jSpVv[3Srb36gZZN{[Xl? MUSyOVAh|ryP M1fsd2ROW09? Mn21ZYN1cX[jdHXzJGFOWEtic3nncoFtcW6pIIDheIh4[Xm| Mn3PNVk5Ojh6M{[=
L6 skeletal muscle cells NXHRcVJkTnWwY4Tpc44h[XO|YYm= MUKyOVAh|ryP NYfEXFNQTE2VTx?= MXfpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= M3vJOVE6QDJ6OEO2
MDA-MB231 NWLVWZNzSXCxcITvd4l{KGG|c3H5 M3LXUlQxOCEQvF2= MVjEUXNQ M1TNZ5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MlrpNVk5QTZ2Nkm=
BT474 M1HsO2Fxd3C2b4Ppd{Bie3OjeR?= NV\RZ|FDPDByIN88US=> M2\QfGROW09? NWXiSop7e2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= M1zBelE6QDl4NE[5
MCF7 MXfBdI9xfG:|aYOgZZN{[Xl? NIP3UlQ1ODBizszN MmXVSG1UVw>? M{XmT5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MonYNVk5QTZ2Nkm=
Mesenchymal stem cells NXj6O2xqU2mwYYPlJIF{e2G7 MV:xNEDDvU1? Mny2SG1UVw>? NHfIO|FqdmS3Y3XzJIEhem:kdYP0JIFv\CC|dYP0ZYlv\WRiQV3QT{Bi[3SrdnH0bY9v NITMV|YzPDFyNEi3PS=>
Mesenchymal stem cells M4frUYN6fG:2b4jpZ4l1gSCjc4PhfS=> MkjqNVAxKML3TR?= M1LMWWROW09? MXjk[YNz\WG|ZYOgeIhmKE2VQzDwdo9tcW[ncnH0bY9v NIjIW5AzPDFyNEi3PS=>
MG-63 MoLwZ5l1d3SxeHnjbZR6KGG|c3H5 NULQeWpUOTBiwsXN M4rNNGROW09? M{jS[YlvcGmkaYTzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhTGWjdHi= NH;MTm4zPDl4MEO2Ni=>
MC3T3-E1 Mmj5Z5l1d3SxeHnjbZR6KGG|c3H5 MlyzNVAhyrWP MkjGSG1UVw>? NGTseIdqdmirYnn0d{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKESnYYTo Mnm4NlQ6PjB|NkK=
MG-63 M1eybWFxd3C2b4Ppd{Bie3OjeR?= M4jUdlExKML3TR?= NF36NWNFVVOR MmDld5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? MX2yOFk3ODN4Mh?=
MC3T3-E1 M3vPZmFxd3C2b4Ppd{Bie3OjeR?= MXKxNEDDvU1? NFrSW3VFVVOR NXjpZXFbe3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= MnThNlQ6PjB|NkK=
MG-63 MX3GeY5kfGmxbjDhd5NigQ>? NGO3XGMyOCEEtV2= NFHSUZFFVVOR MXzhcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? NUDje2VYOjR7NkCzOlI>
MC3T3-E1 M17Ie2Z2dmO2aX;uJIF{e2G7 MmjLNVAhyrWP Mof4SG1UVw>? M4DDboFtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= M3:2elI1QTZyM{[y
MG-63 MkGxSpVv[3Srb36gZZN{[Xl? NYPLU4JmOTBiwsXN NV\BVm9MTE2VTx?= Mnmx[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NYDt[HpMOjR7NkCzOlI>
MC3T3-E1 MWrGeY5kfGmxbjDhd5NigQ>? NETjeHcyOCEEtV2= NXPkVY5iTE2VTx?= Mn6z[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NXfuSG9ROjR7NkCzOlI>
PC3 M4nRWGtqdmG|ZTDhd5NigQ>? M3q5PVExOCEEtV2= M4DPN2ROW09? NYTq[FJ6fXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v NYrVPWZROjV3OUSwOFM>
PC3M MoOzT4lv[XOnIHHzd4F6 M2C2XFExOCEEtV2= MVzEUXNQ MWH1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= NVuyN3VxOjV3OUSwOFM>
PC3 MnjNSpVv[3Srb36gZZN{[Xl? MYWxNFAhyrWP M3TQ[2ROW09? NV3S[GxYcW6mdXPld{BRUTONL33UU3IheGG2aIfhfZM> NV7XeJNZOjV3OUSwOFM>
PC3M MmnXSpVv[3Srb36gZZN{[Xl? MlS3NVAxKML3TR?= NFjmZYZFVVOR M3OxcIlv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz MVeyOVU6PDB2Mx?=
PC3 NIPIR2VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIfHZm4yODBiwsXN MWTEUXNQ NXzTXGRbe3WycILld5NmeyCycn;sbYZmemG2aX;u M1i2XVI2PTl2MESz
PC3M NUPDTXJPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MnrjNVAxKML3TR?= NWDqUlB{TE2VTx?= Mnm0d5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:w M4\STlI2PTl2MESz
MC3T3-E1 NWHM[mVtU2mwYYPlJIF{e2G7 MmnlNVAh|ryP NHHFNWNFVVOR M{C0WYlv\HWlZYOgd4lodmmoaXPhcpQhSU2SSzDhZ5RqfmG2aX;u MYWyOlg6OTh4Nh?=
MC3T3-E1 MnPRS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXWzfGdmOTBizszN NGX0Uo5FVVOR NVnVTm9ScW6qaXLpeJMhTGW6LXnu[JVk\WRib4P0[Y9jdGG|dDDj[YxtKGSnYYTo M3\OV|I3QDlzOE[2
MC3T3-E1 Moi5SpVv[3Srb36gZZN{[Xl? M{XWeFExKM7:TR?= NHzwdmlFVVOR MWTpcohq[mm2czDE[ZgucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz M2TzO|I3QDlzOE[2

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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.

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䲧疝Ỵ疞㧀疜膉痘 瘿뾠ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ€𢡄뙤ෆ€䀷痗뙤ෆ౴뙤ෆ㵶痗뙤ෆ뺖᎒泌

22456226 26431377
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