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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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.

    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.

  • 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.

    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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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]
(Cell-free assay)
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 MWHGeY5kfGmxbjDhd5NigQ>? MoLXNUBuVQ>? MVjEUXNQ MoD6bY5pcWKrdIOg[oF1fHliYXPp[EB{gW62aHXzbZMhf2m2aDDJR|UxKG:oIEOuOkDPxE1? NGHURYQyPjd3M{W3Oi=>
rat hepatocytes MnPjSpVv[3Srb36gZZN{[Xl? NFfabWQyKG2P MV3EUXNQ NVPrOmtvcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= NWn4NlcxOTZ5NUO1O|Y>
HEK293 M{XxNmtqdmG|ZTDhd5NigQ>? NHm0TGszODBizszN M1rFRmROW09? NVr4eIx4[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> NVfJVmRHOTd5MkiyOFE>
CCL13 NWGx[2E4U2mwYYPlJIF{e2G7 M2fHWFIxOCEQvF2= M4TwWmROW09? MYLhZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN MnzGNVc4Ojh{NEG=
MEFs NWGyZmRnTnWwY4Tpc44h[XO|YYm= NUW0PVlvOzByIN88US=> NVPaS5VETE2VTx?= MkDpbY5pcWKrdIOgdJJwfGWjc3;tZYwh\nWwY4Tpc44h[nliYX6gRW1RUy2rbnTldIVv\GWwdDDt[YNp[W6rc32= MVSxPFU6OzV6NB?=
epididymal clear cells MlvhSpVv[3Srb36gZZN{[Xl? M3LKc|IxOCEQvF2= MY\EUXNQ MXLpcohq[mm2czD0bIUheEhvbXXkbYF1\WRiVj3BWHBie2ViYXPjeY12dGG2aX;uJIF1KHSqZTDhdIlk[WxibXXtZpJidmV? NVjwXJVyOTl{MUG5NVg>
3T3-L1 NGiybZJHfW6ldHnvckBie3OjeR?= NHvUSpgyNjJibV2= NVTuOFNQTE2VTx?= NHLQVGhqdmirYnn0d{A{XDNvTEGgRYRqeG:pZX7ld4l{ Moj6NVk1QDN|MES=
3T3-L1 MUTGeY5kfGmxbjDhd5NigQ>? M{XHclEvOiCvTR?= MknLSG1UVw>? MXnpcohq[mm2czD0bIUhTXiycnXzd4lwdiCxZjDB[Ilxd2enbnXzbZNT\WyjdHXkJHRz[W6|Y4LpdJRqd25iRnHjeI9zeyCjbnSgUYFzc2W{cx?= MnfnNVk1QDN|MES=
3T3-L1 NUDpO|A6TnWwY4Tpc44h[XO|YYm= NGqwe|gyNjJibV2= MVrEUXNQ M1;uOYlvcGmkaYTzJG1qfG:2aXOgR4xwdmGuIFX4dIFve2mxbh?= MX:xPVQ5OzNyNB?=
3T3-L1 MnrCZ5l1d3SxeHnjbZR6KGG|c3H5 NYHxWGRvOS5{IH3N NXy0Vmp7TE2VTx?= NX3nbII4\GWlcnXhd4V{KEOnbHygWoli[mmuaYT5 Ml;FNVk1QDN|MES=
3T3-L1 MYfLbY5ie2ViYYPzZZk> NUHa[ZB6OS5{IH3N MVfEUXNQ MXjhZ5RqfmG2ZYOgRW1RUw>? MoXmNVk1QDN|MES=
L6 skeletal muscle cells M4fGcmZ2dmO2aX;uJIF{e2G7 MkXCNlUxKM7:TR?= NETvOoZFVVOR NGT5fXRi[3SrdnH0[ZMhSU2SSzDzbYdv[WyrbnegdIF1cHejeYO= M1LDO|E6QDJ6OEO2
L6 skeletal muscle cells NF3MT|dHfW6ldHnvckBie3OjeR?= Moq2NlUxKM7:TR?= Ml3CSG1UVw>? MV;pcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= NGDRdZgyQTh{OEizOi=>
MDA-MB231 NUHVO3hDSXCxcITvd4l{KGG|c3H5 NF;LW5Y1ODBizszN Mn;BSG1UVw>? M4Xq[JNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MVmxPVg6PjR4OR?=
BT474 NYK0cXFlSXCxcITvd4l{KGG|c3H5 MmPHOFAxKM7:TR?= NEPiU3lFVVOR M1TMOJNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MUmxPVg6PjR4OR?=
MCF7 M4TITGFxd3C2b4Ppd{Bie3OjeR?= NEHGNWg1ODBizszN NUHBbI1lTE2VTx?= Mlnvd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? MlLENVk5QTZ2Nkm=
Mesenchymal stem cells NVzWPJFuU2mwYYPlJIF{e2G7 MkDVNVAhyrWP MmDLSG1UVw>? MmnCbY5lfWOnczDhJJJw[nW|dDDhcoQhe3W|dHHpcoVlKEGPUFugZYN1cX[jdHnvci=> NVXlcXhTOjRzMES4O|k>
Mesenchymal stem cells NUfVd|ZS[3m2b4TvfIlkcXS7IHHzd4F6 MXqxNFAhyrWP MnrTSG1UVw>? NX;h[3ll\GWlcnXhd4V{KHSqZTDNV2MheHKxbHnm[ZJifGmxbh?= MY[yOFExPDh5OR?=
MG-63 M2TGcoN6fG:2b4jpZ4l1gSCjc4PhfS=> MWSxNEDDvU1? NVLrTmJDTE2VTx?= NGPJ[FZqdmirYnn0d{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKESnYYTo MoH0NlQ6PjB|NkK=
MC3T3-E1 Mn\uZ5l1d3SxeHnjbZR6KGG|c3H5 NVXK[Fc1OTBiwsXN NFHZR2xFVVOR NXTsfG51cW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> M2TsOVI1QTZyM{[y
MG-63 MnTSRZBweHSxc3nzJIF{e2G7 MXWxNEDDvU1? MVvEUXNQ MVHzeZBxemW|c3XzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhSXCxcITvd4l{ NHXwW3IzPDl4MEO2Ni=>
MC3T3-E1 NYLJSVV5SXCxcITvd4l{KGG|c3H5 Mom0NVAhyrWP MmjDSG1UVw>? NXWxTYk{e3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= MmnDNlQ6PjB|NkK=
MG-63 MXHGeY5kfGmxbjDhd5NigQ>? NVnTUVlGOTBiwsXN MVfEUXNQ MWThcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? M4OyNFI1QTZyM{[y
MC3T3-E1 MXPGeY5kfGmxbjDhd5NigQ>? MoLtNVAhyrWP NG[5dm5FVVOR MWrhcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? MkHmNlQ6PjB|NkK=
MG-63 NX3nd2hNTnWwY4Tpc44h[XO|YYm= M17K[FExKML3TR?= NYm1PYZnTE2VTx?= MoLK[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NYnibHN6OjR7NkCzOlI>
MC3T3-E1 NWT2cVhXTnWwY4Tpc44h[XO|YYm= MWSxNEDDvU1? NWHGXo11TE2VTx?= MVLmZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36= MmXJNlQ6PjB|NkK=
PC3 Ml3DT4lv[XOnIHHzd4F6 M1n2[VExOCEEtV2= NVPURlROTE2VTx?= MYL1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= M4K0WVI2PTl2MESz
PC3M MU\LbY5ie2ViYYPzZZk> MmKzNVAxKML3TR?= M1OxOmROW09? NIXtW5d2eHKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJGFOWEtiYX7kJGFESyCyaH;zdIhwenmuYYTpc44> NYHJOlJsOjV3OUSwOFM>
PC3 NXzxc2ZtTnWwY4Tpc44h[XO|YYm= NIrQUmUyODBiwsXN M2\WV2ROW09? MoPUbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= M{DjTFI2PTl2MESz
PC3M NFzoUGtHfW6ldHnvckBie3OjeR?= NETTTHgyODBiwsXN MkX0SG1UVw>? NV\KUZhUcW6mdXPld{BRUTONL33UU3IheGG2aIfhfZM> NEi2XVEzPTV7NEC0Ny=>
PC3 NH;DZXZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mof2NVAxKML3TR?= MYrEUXNQ NVXCdHN2e3WycILld5NmeyCycn;sbYZmemG2aX;u NVvGV4FJOjV3OUSwOFM>
PC3M MlzvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX;BNoJFOTByINM1US=> MWnEUXNQ MYPzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? M2f6TFI2PTl2MESz
MC3T3-E1 NFnRO5FMcW6jc3WgZZN{[Xl? NIDzfnUyOCEQvF2= MUjEUXNQ NV\Jb2dvcW6mdXPld{B{cWewaX\pZ4FvfCCDTWDLJIFkfGm4YYTpc44> M3i5[VI3QDlzOE[2
MC3T3-E1 NIDkU5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkL6NVAh|ryP M{fjO2ROW09? MorUbY5pcWKrdIOgSIV5NWmwZIXj[YQhd3O2ZX;icIF{fCClZXzsJIRm[XSq M4X6eVI3QDlzOE[2
MC3T3-E1 MoiySpVv[3Srb36gZZN{[Xl? NWi0S2t4OTBizszN NVLIZlZkTE2VTx?= NWrhfVQ{cW6qaXLpeJMhTGW6LXnu[JVk\WRib4jp[IF1cX[nIIP0doV{ew>? MYqyOlg6OTh4Nh?=

... Click to View More Cell Line Experimental Data

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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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