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A-769662

For research use only.

Catalog No.S2697

45 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 45 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 M2LqVGZ2dmO2aX;uJIF{e2G7 MU[xJI1O MV3EUXNQ M2G5N4lvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP NVX0OY5qOTZ5NUO1O|Y>
rat hepatocytes NVuxWWRHTnWwY4Tpc44h[XO|YYm= NX7lSYR1OSCvTR?= NFnCeoZFVVOR MUDpcohq[mm2czDmZZR1gSCjY3nkJJN6dnSqZYPpd{B4cXSqIFnDOVAhd2ZiMz62JO69VQ>? NIP5[YUyPjd3M{W3Oi=>
HEK293 MYXLbY5ie2ViYYPzZZk> M4e4V|IxOCEQvF2= MkjISG1UVw>? MmX6ZYN1cX[jdHXzJIVv\G:pZX7veZMhSU2SSx?= MUCxO|czQDJ2MR?=
CCL13 MXvLbY5ie2ViYYPzZZk> NIiwXGczODBizszN Mo\VSG1UVw>? MXzhZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN MVKxO|czQDJ2MR?=
MEFs MXXGeY5kfGmxbjDhd5NigQ>? NXTtNHBTOzByIN88US=> NWn1NmF3TE2VTx?= MkHMbY5pcWKrdIOgdJJwfGWjc3;tZYwh\nWwY4Tpc44h[nliYX6gRW1RUy2rbnTldIVv\GWwdDDt[YNp[W6rc32= MV:xPFU6OzV6NB?=
epididymal clear cells MoXrSpVv[3Srb36gZZN{[Xl? M{fRV|IxOCEQvF2= NYrKZW86TE2VTx?= M4HXW4lvcGmkaYTzJJRp\SCySD3t[YRq[XSnZDDWMWFVWGG|ZTDhZ4N2dXWuYYTpc44h[XRidHjlJIFxcWOjbDDt[Y1jemGwZR?= NWrKNlM{OTl{MUG5NVg>
3T3-L1 M3\qeWZ2dmO2aX;uJIF{e2G7 MlvnNU4zKG2P MW\EUXNQ NYD4S5hxcW6qaXLpeJMhO1R|LVyxJGFlcXCxZ3Xu[ZNqew>? MWGxPVQ5OzNyNB?=
3T3-L1 MYrGeY5kfGmxbjDhd5NigQ>? M4D6[FEvOiCvTR?= MkHDSG1UVw>? Mnr4bY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gRYRqeG:pZX7ld4l{WmWuYYTl[EBVemGwc3PybZB1cW:wIF\hZ5RwenNiYX7kJG1iemuncoO= NIjDfIIyQTR6M{OwOC=>
3T3-L1 M1fVeWZ2dmO2aX;uJIF{e2G7 NW\vXHJIOS5{IH3N MXLEUXNQ MnXhbY5pcWKrdIOgUYl1d3SrYzDDcI9v[WxiRYjwZY5{cW:w MknGNVk1QDN|MES=
3T3-L1 MXrjfZRwfG:6aXPpeJkh[XO|YYm= MmrYNU4zKG2P NH[yelFFVVOR MV\k[YNz\WG|ZYOgR4VtdCCYaXHibYxqfHl? NGHWRm0yQTR6M{OwOC=>
3T3-L1 NWPhNm1{U2mwYYPlJIF{e2G7 MUSxMlIhdU1? MoHmSG1UVw>? MUDhZ5RqfmG2ZYOgRW1RUw>? NV3UO5VZOTl2OEOzNFQ>
L6 skeletal muscle cells MmK2SpVv[3Srb36gZZN{[Xl? MUeyOVAh|ryP M{fIXmROW09? NH7adHVi[3SrdnH0[ZMhSU2SSzDzbYdv[WyrbnegdIF1cHejeYO= M3[xUVE6QDJ6OEO2
L6 skeletal muscle cells MVnGeY5kfGmxbjDhd5NigQ>? M1HaTVI2OCEQvF2= M3Hx[GROW09? MX3pcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= MVKxPVgzQDh|Nh?=
MDA-MB231 NECxUXpCeG:ydH;zbZMh[XO|YYm= MlqwOFAxKM7:TR?= MUTEUXNQ MWfz[Y5{cXSrenXzJIh2dWGwIHLy[YF{fCClYX7j[ZIh[2WubDDsbY5meyC2bzDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqew>? NUWyO2Y6OTl6OU[0Olk>
BT474 NGTqb4NCeG:ydH;zbZMh[XO|YYm= MYG0NFAh|ryP NFnhZ5lFVVOR NX\YVIw{e2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= M4PhTVE6QDl4NE[5
MCF7 M4L3ZmFxd3C2b4Ppd{Bie3OjeR?= MXu0NFAh|ryP MX3EUXNQ NYr5bGtSe2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= MnT4NVk5QTZ2Nkm=
Mesenchymal stem cells M1XrUWtqdmG|ZTDhd5NigQ>? M3;MSVExKML3TR?= NFPhNWRFVVOR NXnpVm9tcW6mdXPld{BiKHKxYoXzeEBidmRic4XzeIFqdmWmIFHNVGsh[WO2aY\heIlwdg>? NFjPdYczPDFyNEi3PS=>
Mesenchymal stem cells NEHOT5RkgXSxdH;4bYNqfHliYYPzZZk> NG\NfZIyODBiwsXN NVvBUpgxTE2VTx?= MWLk[YNz\WG|ZYOgeIhmKE2VQzDwdo9tcW[ncnH0bY9v M3myZlI1OTB2OEe5
MG-63 MoKyZ5l1d3SxeHnjbZR6KGG|c3H5 NEfUWGcyOCEEtV2= NH:3cItFVVOR NV;uUIFRcW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> NVLEeVRxOjR7NkCzOlI>
MC3T3-E1 M{f2VIN6fG:2b4jpZ4l1gSCjc4PhfS=> MWKxNEDDvU1? MonvSG1UVw>? NXHGV5pMcW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> Mo\sNlQ6PjB|NkK=
MG-63 MUHBdI9xfG:|aYOgZZN{[Xl? MW[xNEDDvU1? NVfv[IRSTE2VTx?= M3;IVJN2eHC{ZYPz[ZMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCDcH;weI9{cXN? NVnTTG1EOjR7NkCzOlI>
MC3T3-E1 NYTiVYhPSXCxcITvd4l{KGG|c3H5 M4n4e|ExKML3TR?= MoHnSG1UVw>? M4fYOZN2eHC{ZYPz[ZMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCDcH;weI9{cXN? NFv0WoMzPDl4MEO2Ni=>
MG-63 MkO5SpVv[3Srb36gZZN{[Xl? M3PYU|ExKML3TR?= M3TscWROW09? MU\hcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? NX20PXVzOjR7NkCzOlI>
MC3T3-E1 NG\YXmNHfW6ldHnvckBie3OjeR?= MV[xNEDDvU1? MUDEUXNQ NV3GTVZH[WyuZY\pZZRmeyCUT2OgZYNkfW23bHH0bY9vKGGwZDDBWHAh\GWybHX0bY9vKGOjdYPl[EBjgSCKMl:y MXmyOFk3ODN4Mh?=
MG-63 M2HP[mZ2dmO2aX;uJIF{e2G7 M3PD[lExKML3TR?= MlWwSG1UVw>? MlvB[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u MnnVNlQ6PjB|NkK=
MC3T3-E1 NVizT4ppTnWwY4Tpc44h[XO|YYm= NIXseJIyOCEEtV2= M3PuZWROW09? MXfmZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36= MYqyOFk3ODN4Mh?=
PC3 NFPtdm1McW6jc3WgZZN{[Xl? NYrROolbOTByINM1US=> MWfEUXNQ NVTEUHg5fXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v M{DTflI2PTl2MESz
PC3M NX:yT3dNU2mwYYPlJIF{e2G7 MXyxNFAhyrWP M3jvR2ROW09? NEXXSZl2eHKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJGFOWEtiYX7kJGFESyCyaH;zdIhwenmuYYTpc44> MlzGNlU2QTRyNEO=
PC3 NHz2ZWVHfW6ldHnvckBie3OjeR?= NXP6ZoNLOTByINM1US=> NEfZcWNFVVOR NVPGfFdrcW6mdXPld{BRUTONL33UU3IheGG2aIfhfZM> NIfE[ZEzPTV7NEC0Ny=>
PC3M M2jGdGZ2dmO2aX;uJIF{e2G7 Ml3UNVAxKML3TR?= M2PkPWROW09? NHrIOJJqdmS3Y3XzJHBKO0txbWTPVkBx[XSqd3H5dy=> MoHlNlU2QTRyNEO=
PC3 M3fRd2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3fXeVExOCEEtV2= NV[0cGNDTE2VTx?= MV7zeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? M3rE[VI2PTl2MESz
PC3M MlfuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NUexemR1OTByINM1US=> MmjPSG1UVw>? NHX4[5V{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36= MV6yOVU6PDB2Mx?=
MC3T3-E1 NWnxTFNFU2mwYYPlJIF{e2G7 NGHyNFQyOCEQvF2= MnXxSG1UVw>? NFzocGFqdmS3Y3XzJJNq\26rZnnjZY51KEGPUFugZYN1cX[jdHnvci=> NHvabmYzPjh7MUi2Oi=>
MC3T3-E1 MYLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXLUWWJtOTBizszN NIHGSHVFVVOR MUfpcohq[mm2czDE[ZgucW6mdXPl[EBwe3Snb3LsZZN1KGOnbHyg[IVifGh? M{TqNFI3QDlzOE[2
MC3T3-E1 NGjY[YtHfW6ldHnvckBie3OjeR?= NXrD[FNTOTBizszN NVvwUGxKTE2VTx?= MYfpcohq[mm2czDE[ZgucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz MofXNlY5QTF6Nk[=

... 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