MK8722 |
رقم الكتالوجGC31470
One-Click Copy Product Info
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MK8722 هو منشط قوي ومنظم لعموم AMPK
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1394371-71-1
Sample solution is provided at 25 µL, 10mM.
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MK8722 is an orally allosteric pan-AMPK activator that supports glucose homeostasis, with EC50 values of 1-60nM[1]. MK8722 binds to the allosteric drug and metabolite (ADaM) site between the α-kinase domain and the β-glycogen-binding domain, stabilizes the enzyme’s activation loop in an active conformation, and allows bypassing the need for AMPKα T172 phosphorylation for full enzyme activation [2]. MK8722 has been widely used in animal models to regulate blood glucose levels and glucose uptake[3].
In vitro, MK8722 treatment for 48h significantly inhibited the proliferation of A2780, OV90, and SKOV3 cells with IC50 values of 35.47, 36.44 and 47.89μg/ml, respectively[4]. Treatment of PANC-1 cells with 50μM MK8722 for 24h significantly reduced colony formation and inhibited cell invasion and migration[5]. Pretreatment with 10μM MK8722 for 30min reduced the abundance of Bax, Caspase-3, and the Bax/Bcl-2 ratio and increased the abundance of SIRT3 and MnSOD activity in H2O2-induced bovine mammary alveolar cells (MAC-T)[6].
In vivo, MK8722 treatment via daily subcutaneous injection at a dose of 30mg/kg for 4 weeks in 4-month-old male HSALR mice improved the alternative splicing of Atp2a1 in the tibialis anterior muscle and resulted in the activation of AMPK and a switch of oxidative metabolism[7]. Daily oral administration of MK8722 at a dose of 30mg/kg for 30 days attenuated paclitaxel-induced hyperalgesia in male and female mice[8].
References:
[1] Myers R W, Guan H P, Ehrhart J, et al. Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy[J]. Science, 2017, 357(6350): 507-511.
[2] Doshi H, Spengler K, Godbole A, et al. AMPK protects endothelial cells against HSV-1 replication via inhibition of mTORC1 and ACC1[J]. Microbiology Spectrum, 2023, 11(5): e00417-23.
[3] Feng D, Biftu T, Romero F A, et al. Discovery of MK-8722: a systemic, direct pan-activator of AMP-activated protein kinase[J]. ACS medicinal chemistry letters, 2018, 9(1): 39-44.
[4] Wang L, Zhu H, Shi Z, et al. MK8722 initiates early-stage autophagy while inhibiting late-stage autophagy via FASN-dependent reprogramming of lipid metabolism[J]. Theranostics, 2024, 14(1): 75.
[5] Wang C, Huang B, Sun L, et al. MK8722, an AMPK activator, inhibiting carcinoma proliferation, invasion and migration in human pancreatic cancer cells[J]. Biomedicine & Pharmacotherapy, 2021, 144: 112325.
[6] Liu L, Lu O, Li D, et al. Sirtuin 3 mitigates oxidative-stress-induced apoptosis in bovine mammary epithelial cells[J]. Journal of Dairy Science, 2023, 106(10): 7266-7280.
[7] Ravel‐Chapuis A, Fahmi C, Gobin J, et al. The AMPK allosteric activator MK‐8722 improves the histology and spliceopathy in myotonic dystrophy type 1 (DM1) skeletal muscle[J]. The FASEB Journal, 2024, 38(23): e70199.
[8] Inyang K E, McDougal T A, Ramirez E D, et al. Alleviation of paclitaxel-induced mechanical hypersensitivity and hyperalgesic priming with AMPK activators in male and female mice[J]. Neurobiology of Pain, 2019, 6: 100037.
| Cell experiment [1]: | |
Cell lines | A2780 cells |
Preparation Method | A2780 cells were cultured in complete Dulbecco's modified Eagle's medium (DMEM) supplemented with 100µg/ml streptomycin, 100U/ml penicillin, and 10% fetal bovine serum (FBS) at 37°C in 5% CO2. Cells were seeded in 96-well plates at a density of approximately 3×103 cells/well and incubated for 24 hours. Subsequently, cells were treated with MK8722 (5, 10, 20, 40, 60, 80, and 100μM) for 48 hours. The CCK-8 solution was diluted in the medium at a ratio of 1:10 and added to a 96-well plate. After 2h of incubation, cell viability was determined. |
Reaction Conditions | 5, 10, 20, 40, 60, 80, and 100μM; 48h |
Applications | MK8722 treatment inhibited the cell viability of A2780 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BALB/c nude mice |
Preparation Method | Male nude mice (BALB/c), weighing 18-22g, aged 6-8 weeks, were housed in a temperature, humidity, and light-controlled environment and fed a standard mouse diet and water. Experimental mice (n=3) were subcutaneously injected with 5×106 PANC-1 cells dissolved in 100μl PBS into the root of the right lower limb, followed by daily gavage of MK8722 (25mg/kg/day) for 30 days. Control mice (n=3) were injected with 5×106 PANC-1 cells and gavaged with control vehicle (DMSO) daily. Tumor length and width were measured every other day, and tumor volume was calculated using the formula V=(length×width2)/2, where length was always the longest dimension of the tumor. |
Dosage form | 25mg/kg/day for 30 days; p.o. |
Applications | MK8722 treatment significantly inhibited tumor volume and weight in mice. |
References: | |
| Cas No. | 1394371-71-1 | SDF | |
| Canonical SMILES | O[C@H]1[C@@]([C@]2([H])OC1)([H])OC[C@H]2OC3=NC4=NC(C(C=C5)=CC=C5C6=CC=CC=C6)=C(Cl)C=C4N3 | ||
| Formula | C24H20ClN3O4 | M.Wt | 449.89 |
| الذوبان | DMSO : ≥ 62.5 mg/mL (138.92 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2228 mL | 11.1138 mL | 22.2277 mL |
| 5 mM | 444.6 μL | 2.2228 mL | 4.4455 mL |
| 10 mM | 222.3 μL | 1.1114 mL | 2.2228 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)