2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. A-769662

A-769662 is a AMP-activated protein kinase (AMPK) activator. A-769662 inhibits the function of the 26S proteasome by an AMPK-independent mechanism and leads to cell cycle arrest. A-769662 directly stimulates partially purified rat liver AMPK (EC50 = 0.8 μM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 μM). A-769662 can alleviate the symptoms of metabolic diseases such as type 2 diabetes.

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A-769662 Chemical Structure

A-769662 Chemical Structure

CAS No. : 844499-71-4

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Based on 42 publication(s) in Google Scholar

A-769662 Related Antibodies

Top Publications Citing Use of Products

40 Publications Citing Use of MCE A-769662

WB

    A-769662 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2017 Oct 19;68(2):336-349.e6.  [Abstract]

    AMPK DKO SV40-immortalized MEFs are electroporated with plasmids encoding Myc-tagged AMPK α1, Myc-tagged AMPK α2 and Myc-tagged AMPK α2 S > A. 48 hr later, MEFs are starved for 3 hr and treated for 2 hr with DMSO or 50 mM A769662 before protein extraction. Western blot analysis shows the A769662-induced ACC phosphorylation in transfected cells.

    A-769662 purchased from MedChemExpress. Usage Cited in: Mol Neurobiol. 2017 Apr;54(3):2301-2312.  [Abstract]

    Effect of A769662 on high glucose-induced inflammatory changes in N2A cells and inflammatory marker expression in sciatic nerves of STZ induced rats. Representative immunoblot images of iNOS, COX-2, NF-κB, β-actin and corresponding graphical representations of densitometric analysis.

    View All AMPK Isoform Specific Products:

    View All Isoforms
    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    A-769662 is a AMP-activated protein kinase (AMPK) activator. A-769662 inhibits the function of the 26S proteasome by an AMPK-independent mechanism and leads to cell cycle arrest. A-769662 directly stimulates partially purified rat liver AMPK (EC50 = 0.8 μM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 μM). A-769662 can alleviate the symptoms of metabolic diseases such as type 2 diabetes[1][2][3][4].

    IC50 & Target[1]

    AMPK

    0.8 μM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    Hepatocyte IC50
    3.2 μM
    Compound: 2, A-769662
    Activation of AMPK in rat primary hepatocytes assessed as inhibition of fatty acid biosynthesis by 14C-acetate incorporation assay
    Activation of AMPK in rat primary hepatocytes assessed as inhibition of fatty acid biosynthesis by 14C-acetate incorporation assay
    		[PMID: 24900695]
    In Vitro

    A-769662 (0.1-100 μM) increases AMPK activity in the presence of a saturating concentration of AMP (300 μM)[1].
    A-769662 (1 nM-1 mM, 4h) increases acetyl-CoA carboxylase (ACC) phosphorylation dose-dependently in primary rat hepatocytes[1].
    A-769662 (50-300 μM, 1 h) increases the GFP-dependent fluorescence dose-dependently in HEK-GFPu-1 cells[3].
    A-769662 (0-50 μM, 1 h) is able to reduce the activity of pre-existing proteasomal activity in MEF cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    A-769662 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: Primary rat hepatocytes
    Concentration: Primary rat hepatocytes
    Incubation Time: 4 h
    Result: Increased ACC phosphorylation dose-dependently.
    Showed that increased ACC phosphorylation correlated with inhibition of fatty acid synthesis as measured by incorporation of 14C-acetate into fatty acids with IC50 of 3.2 μM.
    In Vivo

    A-769662 (30 mg/kg, i.p., single dose) significantly reduces the respiratory exchange ratio relative to vehicle, indicating increased fatty acid utilization despite the availability of carbohydrates in Sprague Dawley rats[1].
    A-769662 (3-30 mg/kg, i.p., b.i.d., for 5 d) reduces plasma glucose levels, lipids, and ACC activity in ob/ob and lean littermate mice[1].
    A-769662 (3-30 mg/kg, i.p., b.i.d., for 14 d) reduces plasma glucose in ob/ob and lean littermate mice[1].
    A-769662 (10-300 μM, 1 h) inhibits the proteasomal function in mouse embryonic fibroblast (MEF) cells with an IC50 of 62 μM in wild-type and double α1 -/- α1 -/- KO mice [3].
    A-769662 (300 μM) has toxic effects on MEF cells in wild-type and double α1 -/- α1 -/- KO mice[3].
    A-769662 (15-30 mg/kg, i.p., 2 w) induces AMPK activation that normalizes the nerve functional changes and reduces pain associated with diabetic neuropathy (DN) in diabetic mice[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Sprague Dawley rats fed ad libitum prior were first acclimated by placing them in a gas exchange indirect calorimeter without food for 2 h then gavaged with a mixed meal plus A-769662[1]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection (i.p.), single dose
    Result: Resulted in 33% reduction of malonyl CoA levels in livers of treated animals in relative to the vehicle.
    Had a statistically nonsignificant decrease in malonyl CoA levels in skeletal muscle of rats treated with A-769662.
    Animal Model: 6- to 7-weeks-old ob/ob and lean littermate mice[3]
    Dosage: 3 or 30 mg/kg b.i.d. for 5 days; 3, 10, or 30 mg/kg b.i.d. for 14 days
    Administration: Intraperitoneal injection (i.p.)
    Result: Significantly decreases fed plasma glucose (30-40% reduction) at 30 mg/kg in both 5 d and 14 d studies.
    Reduced 42% of the fed glucose levels (16 h postdose) in the 5 day study.
    Resulted in a modest reduction in body weight gain in ob/ob mice treated with 30 mg/kg dose for 5 days.
    Resulted in a transient reduction in food intake in the 14 d study.
    Increased the compound concentrations in liver 1 h after 30 or 3 mg/kg of A-769662 approximately 30-fold or 2.5-fold above the cellular IC50 for fatty acid synthesis.
    Animal Model: Healthy male Sprague-Dawley rats (250-270 g) fed on standard diet and water ad libitum then induced diabetes with Streptozotocin (HY-13753) (55 mg/kg, i.p.)[4]
    Dosage: 15 or 30 mg/kg for 14 days
    Administration: Intraperitoneal injection (i.p.)
    Result: Attenuated the pain hypersensitivity and resulted in improved tail flick latencies and paw withdrawal threshold.
    Resulted in marked reduction in motor/sensory nerve conduction velocities (MNCV and SNCV) as well as restoring impaired nerve blood flow (NBF).
    Significantly reduced TUNEL-positive cells, inhibited the lipid peroxidation and improved the antioxidant defence by improving glutathione levels in the sciatic nerves of treated diabetes rats.
    Significantly reduces the expression of IL-6 and TNF-α and reduced the expression of NF-κB and COX-2 compared to diabetic rats.
    Reversed AMPK inactivation and associated mitochondrial biogenesis and autophagy deficits in diabetic rats.
    Significantly elevated mitochondrial ATP production in treated rats.
    Molecular Weight

    360.39

    Formula

    C20H12N2O3S
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    N#CC1C(C2=C(NC1=O)SC=C2C3=CC=C(C4=CC=CC=C4O)C=C3)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (138.74 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7748 mL 13.8739 mL 27.7477 mL
    5 mM 0.5550 mL 2.7748 mL 5.5495 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.33%

    SDS (393 KB)

    COA (259 KB) HNMR (288 KB) RP-HPLC (282 KB) MS (69 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7748 mL 13.8739 mL 27.7477 mL 69.3693 mL
    5 mM 0.5550 mL 2.7748 mL 5.5495 mL 13.8739 mL
    10 mM 0.2775 mL 1.3874 mL 2.7748 mL 6.9369 mL
    15 mM 0.1850 mL 0.9249 mL 1.8498 mL 4.6246 mL
    20 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4685 mL
    25 mM 0.1110 mL 0.5550 mL 1.1099 mL 2.7748 mL
    30 mM 0.0925 mL 0.4625 mL 0.9249 mL 2.3123 mL
    40 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
    50 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3874 mL
    60 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
    80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
    100 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
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    A-769662 Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    A-769662844499-71-4A769662A 769662AMPKAMP-activated protein kinase26S proteasomecell cycle arresttype 2 diabetesInhibitorinhibitorinhibit

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