A-769662

For research use only.

Catalog No.S2697

38 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 38 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 MX;GeY5kfGmxbjDhd5NigQ>? M{DLc|EhdU1? MYjEUXNQ Mo\6bY5pcWKrdIOg[oF1fHliYXPp[EB{gW62aHXzbZMhf2m2aDDJR|UxKG:oIEOuOkDPxE1? M1f3OVE3PzV|NUe2
rat hepatocytes NEi3OnpHfW6ldHnvckBie3OjeR?= NUnIN|lPOSCvTR?= MorFSG1UVw>? M13Yd4lvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP MVuxOlc2OzV5Nh?=
HEK293 MnHxT4lv[XOnIHHzd4F6 MnXqNlAxKM7:TR?= M2fOdGROW09? NUfyVXc5[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> MnjnNVc4Ojh{NEG=
CCL13 M4rufWtqdmG|ZTDhd5NigQ>? NYHjUGV4OjByIN88US=> NEL3[Y5FVVOR MU\hZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN MmL2NVc4Ojh{NEG=
MEFs MnLiSpVv[3Srb36gZZN{[Xl? NH\Lcoo{ODBizszN NH35WnJFVVOR NHWyW4hqdmirYnn0d{Bxem:2ZXHzc41idCCodX7jeIlwdiCkeTDhckBCVVCNLXnu[IVx\W6mZX70JI1m[2ijbnnzcS=> NFrJVooyQDV7M{W4OC=>
epididymal clear cells MXrGeY5kfGmxbjDhd5NigQ>? NWLieHBmOjByIN88US=> M2LoeGROW09? NX34V5RUcW6qaXLpeJMhfGinIIDIMY1m\GmjdHXkJHYuSVSSYYPlJIFk[3WvdXzheIlwdiCjdDD0bIUh[XCrY3HsJI1mdWK{YX7l NYf5U2R1OTl{MUG5NVg>
3T3-L1 Mnz2SpVv[3Srb36gZZN{[Xl? NWr2b3NXOS5{IH3N MWjEUXNQ MYHpcohq[mm2czCzWFMuVDFiQXTpdI9o\W6nc3nz M1fvOVE6PDh|M{C0
3T3-L1 MVXGeY5kfGmxbjDhd5NigQ>? NYDyWJNjOS5{IH3N MofRSG1UVw>? NWf2RYlbcW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhSWSrcH;n[Y5me2m|UnXsZZRm\CCWcnHud4NzcXC2aX;uJGZi[3SxcoOgZY5lKE2jcnvldpM> M2ThbVE6PDh|M{C0
3T3-L1 M2W1dWZ2dmO2aX;uJIF{e2G7 M3zaTFEvOiCvTR?= M2TYXGROW09? NUHMcVRvcW6qaXLpeJMhVWm2b4TpZ{BEdG:wYXygSZhx[W6|aX;u MljLNVk1QDN|MES=
3T3-L1 NW\DeZZH[3m2b4TvfIlkcXS7IHHzd4F6 MUixMlIhdU1? MoLESG1UVw>? MXrk[YNz\WG|ZYOgR4VtdCCYaXHibYxqfHl? NG\kd3UyQTR6M{OwOC=>
3T3-L1 M3LqT2tqdmG|ZTDhd5NigQ>? M1XNXFEvOiCvTR?= M4nqd2ROW09? NXHnNIFE[WO2aY\heIV{KEGPUFu= MV2xPVQ5OzNyNB?=
L6 skeletal muscle cells M3mzXWZ2dmO2aX;uJIF{e2G7 M4nZUVI2OCEQvF2= Ml7mSG1UVw>? NWLUco1y[WO2aY\heIV{KEGPUFugd4lodmGuaX7nJJBifGi5YYnz MlTqNVk5Ojh6M{[=
L6 skeletal muscle cells NYDNe5NpTnWwY4Tpc44h[XO|YYm= MYiyOVAh|ryP NY\xemtxTE2VTx?= M3[0fIlvcGmkaYTzJJRp\SCQYTutT{suSVSSYYPlJJRz[W6|cH;yeEBi[3Srdnn0fUBidmRiY3XscEB{fXKoYXPlJIFjfW6mYX7j[S=> M3vQOVE6QDJ6OEO2
MDA-MB231 NVnG[GpiSXCxcITvd4l{KGG|c3H5 NX3FSlNpPDByIN88US=> M{HtdWROW09? NV;QcpZXe2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= NV7XWmJXOTl6OU[0Olk>
BT474 NWjI[VBtSXCxcITvd4l{KGG|c3H5 NH[1bIU1ODBizszN M{jpcGROW09? M1rlVJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| NGLUWncyQTh7NkS2PS=>
MCF7 MnTCRZBweHSxc3nzJIF{e2G7 NXfpOnhSPDByIN88US=> NHHUNoFFVVOR MoPKd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? MlLuNVk5QTZ2Nkm=
Mesenchymal stem cells NFLLRZJMcW6jc3WgZZN{[Xl? MYGxNEDDvU1? NIP5V2xFVVOR MWHpcoR2[2W|IHGgdo9jfXO2IHHu[EB{fXO2YXnu[YQhSU2SSzDhZ5RqfmG2aX;u MlLCNlQyODR6N{m=
Mesenchymal stem cells MmfjZ5l1d3SxeHnjbZR6KGG|c3H5 NXf2e2JiOTByINM1US=> NGr6SIVFVVOR NV;ROXJL\GWlcnXhd4V{KHSqZTDNV2MheHKxbHnm[ZJifGmxbh?= M37CU|I1OTB2OEe5
MG-63 MUDjfZRwfG:6aXPpeJkh[XO|YYm= MWGxNEDDvU1? NVv4WFVnTE2VTx?= NHjqdI9qdmirYnn0d{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKESnYYTo M3;0N|I1QTZyM{[y
MC3T3-E1 NGroNlhkgXSxdH;4bYNqfHliYYPzZZk> MkjaNVAhyrWP NWT1Z3NbTE2VTx?= M3;GSYlvcGmkaYTzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhTGWjdHi= M4DYOVI1QTZyM{[y
MG-63 NVHndWVuSXCxcITvd4l{KGG|c3H5 MljpNVAhyrWP MlLvSG1UVw>? NYG5[VY1e3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= M1TjflI1QTZyM{[y
MC3T3-E1 MYXBdI9xfG:|aYOgZZN{[Xl? NIm1UJYyOCEEtV2= M1zi[GROW09? NGDOcZB{fXCycnXzd4V{KEh{T{KtTY5lfWOnZDDPd5Rmd2KuYYP0JGNmdGxiQYDvdJRwe2m| MYKyOFk3ODN4Mh?=
MG-63 M1qwUWZ2dmO2aX;uJIF{e2G7 M4CyflExKML3TR?= NFnxfVRFVVOR Mn;5ZYxt\X[rYYTld{BTV1NiYXPjeY12dGG2aX;uJIFv\CCDVGCg[IVxdGW2aX;uJINifXOnZDDifUBJOk9{ MV2yOFk3ODN4Mh?=
MC3T3-E1 NYDlfVlWTnWwY4Tpc44h[XO|YYm= Mo\xNVAhyrWP NEXCdFhFVVOR M3XZNYFtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= MYeyOFk3ODN4Mh?=
MG-63 Mo\5SpVv[3Srb36gZZN{[Xl? MmrPNVAhyrWP NWjk[WNJTE2VTx?= NEntd5pn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> MmPoNlQ6PjB|NkK=
MC3T3-E1 NW[2V2h7TnWwY4Tpc44h[XO|YYm= NEG0e4QyOCEEtV2= M1rCSWROW09? MmSy[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NE\wNHozPDl4MEO2Ni=>
PC3 NVjjUmFUU2mwYYPlJIF{e2G7 MoPWNVAxKML3TR?= M2TPRmROW09? MmTpeZBz\We3bHH0[ZMhfGinIHzleoVteyCxZjDBUXBMKGGwZDDBR2MheGixc4Doc5J6dGG2aX;u NHT4TVUzPTV7NEC0Ny=>
PC3M MoHpT4lv[XOnIHHzd4F6 MnT0NVAxKML3TR?= MVfEUXNQ MVX1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= MXuyOVU6PDB2Mx?=
PC3 NGjUe3ZHfW6ldHnvckBie3OjeR?= NWnSfFB1OTByINM1US=> MYDEUXNQ M2jTfolv\HWlZYOgVGk{Uy:vVF;SJJBifGi5YYnz M33TW|I2PTl2MESz
PC3M MYnGeY5kfGmxbjDhd5NigQ>? NWjDVYwzOTByINM1US=> NHuzUY9FVVOR Mo\hbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= MXSyOVU6PDB2Mx?=
PC3 NUPjOppoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVTvR5U{OTByINM1US=> MnjtSG1UVw>? M1fleZN2eHC{ZYPz[ZMheHKxbHnm[ZJifGmxbh?= NEjob3gzPTV7NEC0Ny=>
PC3M M{nYc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MofvNVAxKML3TR?= NUPWNWtnTE2VTx?= MlLsd5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:w MYOyOVU6PDB2Mx?=
MC3T3-E1 NEPZPWRMcW6jc3WgZZN{[Xl? M{PEO|ExKM7:TR?= M3uwTWROW09? NY\JdFM2cW6mdXPld{B{cWewaX\pZ4FvfCCDTWDLJIFkfGm4YYTpc44> NF3KS4szPjh7MUi2Oi=>
MC3T3-E1 MkT5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MknQNVAh|ryP NFzieY1FVVOR MV3pcohq[mm2czDE[ZgucW6mdXPl[EBwe3Snb3LsZZN1KGOnbHyg[IVifGh? MnXxNlY5QTF6Nk[=
MC3T3-E1 MYPGeY5kfGmxbjDhd5NigQ>? NY\VWY9UOTBizszN NVHGVoJrTE2VTx?= MX;pcohq[mm2czDE[ZgucW6mdXPl[EBwgGmmYYTpeoUhe3S{ZYPz NEfuNWEzPjh7MUi2Oi=>

... 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