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.

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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

Choose Selective AMPK Inhibitors

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 NFXLR5ZHfW6ldHnvckBie3OjeR?= M1j0elEhdU1? NEm4OpRFVVOR NWW4N5pkcW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2= M{DvOFE3PzV|NUe2
rat hepatocytes MXvGeY5kfGmxbjDhd5NigQ>? MlW2NUBuVQ>? M3rmXGROW09? M3\N[YlvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryP MV:xOlc2OzV5Nh?=
HEK293 NV:1SIpIU2mwYYPlJIF{e2G7 NV\Bc5JUOjByIN88US=> MXrEUXNQ NG\ndFBi[3SrdnH0[ZMh\W6mb3flco92eyCDTWDL Mmi0NVc4Ojh{NEG=
CCL13 M17uR2tqdmG|ZTDhd5NigQ>? NHvZeIczODBizszN NULOWXNbTE2VTx?= NF\iXZRi[3SrdnH0[ZMh\W6mb3flco92eyCDTWDL M3XBOlE4PzJ6MkSx
MEFs M1rlfWZ2dmO2aX;uJIF{e2G7 MXezNFAh|ryP MkHpSG1UVw>? MWXpcohq[mm2czDwdo91\WG|b33hcEBnfW6ldHnvckBjgSCjbjDBUXBMNWmwZHXw[Y5l\W62IH3lZ4hidmm|bR?= NWPtXlZzOTh3OUO1PFQ>
epididymal clear cells MX;GeY5kfGmxbjDhd5NigQ>? MV6yNFAh|ryP MWXEUXNQ MojLbY5pcWKrdIOgeIhmKHCKLX3l[IlifGWmIG[tRXRR[XOnIHHjZ5VufWyjdHnvckBifCC2aHWgZZBq[2GuIH3lcYJz[W6n MUKxPVIyOTlzOB?=
3T3-L1 NV7mdpU6TnWwY4Tpc44h[XO|YYm= NYT0T3NuOS5{IH3N NInIbYpFVVOR NIjyN|lqdmirYnn0d{A{XDNvTEGgRYRqeG:pZX7ld4l{ MoTmNVk1QDN|MES=
3T3-L1 NH33WJpHfW6ldHnvckBie3OjeR?= MV[xMlIhdU1? M2jORmROW09? MlO4bY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gRYRqeG:pZX7ld4l{WmWuYYTl[EBVemGwc3PybZB1cW:wIF\hZ5RwenNiYX7kJG1iemuncoO= MVOxPVQ5OzNyNB?=
3T3-L1 MYjGeY5kfGmxbjDhd5NigQ>? MYKxMlIhdU1? NEPUcm5FVVOR Mn;zbY5pcWKrdIOgUYl1d3SrYzDDcI9v[WxiRYjwZY5{cW:w M2\tfVE6PDh|M{C0
3T3-L1 MX\jfZRwfG:6aXPpeJkh[XO|YYm= NGnIO5kyNjJibV2= NE[yc45FVVOR NGrzTWdl\WO{ZXHz[ZMhS2WubDDWbYFjcWyrdIm= MU[xPVQ5OzNyNB?=
3T3-L1 M2DucWtqdmG|ZTDhd5NigQ>? M{ntWVEvOiCvTR?= M1fqTmROW09? NXTCUJNt[WO2aY\heIV{KEGPUFu= NXvGPVhMOTl2OEOzNFQ>
L6 skeletal muscle cells M4W4XWZ2dmO2aX;uJIF{e2G7 MlrNNlUxKM7:TR?= M4XiPGROW09? NUH4OmJM[WO2aY\heIV{KEGPUFugd4lodmGuaX7nJJBifGi5YYnz MkPxNVk5Ojh6M{[=
L6 skeletal muscle cells NHGze2ZHfW6ldHnvckBie3OjeR?= Mn\XNlUxKM7:TR?= NXnMepVuTE2VTx?= MXnpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= NYPH[lR3OTl6Mki4N|Y>
MDA-MB231 MYDBdI9xfG:|aYOgZZN{[Xl? MVm0NFAh|ryP NWL3U2pRTE2VTx?= MkPYd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? M1vsOVE6QDl4NE[5
BT474 MY\BdI9xfG:|aYOgZZN{[Xl? NIj2cYo1ODBizszN NWfLeVI4TE2VTx?= MorUd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? Ml;JNVk5QTZ2Nkm=
MCF7 MlLuRZBweHSxc3nzJIF{e2G7 NHuxTZg1ODBizszN MVfEUXNQ NI\me5J{\W6|aYTpfoV{KGi3bXHuJIJz\WG|dDDjZY5k\XJiY3XscEBtcW6nczD0c{BVWkGLTD3pcoR2[2WmIHHwc5B1d3Orcx?= NHXTTXQyQTh7NkS2PS=>
Mesenchymal stem cells MV3LbY5ie2ViYYPzZZk> NWPOblBbOTBiwsXN M1TJe2ROW09? MmjQbY5lfWOnczDhJJJw[nW|dDDhcoQhe3W|dHHpcoVlKEGPUFugZYN1cX[jdHnvci=> NV\TN|B[OjRzMES4O|k>
Mesenchymal stem cells MXjjfZRwfG:6aXPpeJkh[XO|YYm= M{nkcFExOCEEtV2= NXXCe25NTE2VTx?= MofL[IVkemWjc3XzJJRp\SCPU1OgdJJwdGmoZYLheIlwdg>? MoTMNlQyODR6N{m=
MG-63 M3vNWYN6fG:2b4jpZ4l1gSCjc4PhfS=> NVnySG1UOTBiwsXN M3[wUWROW09? MWnpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq NXe2T|ZFOjR7NkCzOlI>
MC3T3-E1 NEHFeYlkgXSxdH;4bYNqfHliYYPzZZk> MVOxNEDDvU1? MXHEUXNQ M3rEcIlvcGmkaYTzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhTGWjdHi= MlnNNlQ6PjB|NkK=
MG-63 NWfuWGp4SXCxcITvd4l{KGG|c3H5 NYfPUIoxOTBiwsXN M2TQdWROW09? NXKyZYVqe3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= NV[0ZXFkOjR7NkCzOlI>
MC3T3-E1 Mk\BRZBweHSxc3nzJIF{e2G7 MUCxNEDDvU1? MX7EUXNQ MY\zeZBxemW|c3XzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhSXCxcITvd4l{ NVXWXZJMOjR7NkCzOlI>
MG-63 NU\wfGwzTnWwY4Tpc44h[XO|YYm= M2LxT|ExKML3TR?= NX7OW4s5TE2VTx?= NETwV|hidGyndnnheIV{KFKRUzDhZ4N2dXWuYYTpc44h[W6mIFHUVEBl\XCuZYTpc44h[2G3c3XkJIJ6KEh{T{K= NFvNc4IzPDl4MEO2Ni=>
MC3T3-E1 NFHGZZpHfW6ldHnvckBie3OjeR?= NFjYb|gyOCEEtV2= NELpSYFFVVOR Mm\OZYxt\X[rYYTld{BTV1NiYXPjeY12dGG2aX;uJIFv\CCDVGCg[IVxdGW2aX;uJINifXOnZDDifUBJOk9{ MXKyOFk3ODN4Mh?=
MG-63 MXnGeY5kfGmxbjDhd5NigQ>? NXXic5BXOTBiwsXN NWfHNHN2TE2VTx?= MkC3[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NEP6PWQzPDl4MEO2Ni=>
MC3T3-E1 NIHmcpRHfW6ldHnvckBie3OjeR?= NUHwXJhnOTBiwsXN M4i0d2ROW09? NIXYR49n[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> NIfudFczPDl4MEO2Ni=>
PC3 NYKwTHRIU2mwYYPlJIF{e2G7 NVrZfHF3OTByINM1US=> NWjYWm55TE2VTx?= NXH1NGxPfXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v MmPjNlU2QTRyNEO=
PC3M MnvwT4lv[XOnIHHzd4F6 NGDWfXcyODBiwsXN NGfE[4lFVVOR MUX1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= M2XEe|I2PTl2MESz
PC3 NVfUV297TnWwY4Tpc44h[XO|YYm= MUWxNFAhyrWP MV\EUXNQ Mn70bY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= M3nkdlI2PTl2MESz
PC3M M2r0T2Z2dmO2aX;uJIF{e2G7 MWixNFAhyrWP NInh[nBFVVOR NGDYN49qdmS3Y3XzJHBKO0txbWTPVkBx[XSqd3H5dy=> Mke1NlU2QTRyNEO=
PC3 M3LEOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFPRXVcyODBiwsXN M2DLVWROW09? NYW3SphMe3WycILld5NmeyCycn;sbYZmemG2aX;u M330c|I2PTl2MESz
PC3M NUnEToNnT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVKxNFAhyrWP MV\EUXNQ MWrzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? NIjvT3UzPTV7NEC0Ny=>
MC3T3-E1 MnzXT4lv[XOnIHHzd4F6 MlmzNVAh|ryP NXrkT3d6TE2VTx?= M{LJVolv\HWlZYOgd4lodmmoaXPhcpQhSU2SSzDhZ5RqfmG2aX;u NIHoWmMzPjh7MUi2Oi=>
MC3T3-E1 M4G3bWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFXLW5EyOCEQvF2= MXHEUXNQ MYjpcohq[mm2czDE[ZgucW6mdXPl[EBwe3Snb3LsZZN1KGOnbHyg[IVifGh? M1XHeFI3QDlzOE[2
MC3T3-E1 M3\R[mZ2dmO2aX;uJIF{e2G7 Ml\BNVAh|ryP Ml3xSG1UVw>? Mof6bY5pcWKrdIOgSIV5NWmwZIXj[YQhd3irZHH0bZZmKHO2cnXzdy=> NVW2Um91OjZ6OUG4OlY>

... 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 slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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