2. Epigenetics PI3K/Akt/mTOR Apoptosis
  3. AMPK mTOR Apoptosis
  4. MT 63-78

MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.

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MT 63-78 Chemical Structure

MT 63-78 Chemical Structure

CAS No. : 1179347-65-9

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MT 63-78 Related Antibodies

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Description

MT 63-78 is a specific and potent direct AMPK activator with an EC50 of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects[1].

IC50 & Target[1]

AMPK

25 μM (EC50)

mTORC1

 

In Vitro

MT 63-78 (0-50 μM; 4 days; LNCaP and PC3 cells) treatment shows a dose-dependent decrease in cell number, and concomitant to the activation of AMPK signaling[1].
MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population[1].
MT 63-78 (0-50 μM; 24 hours; LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells) treatment induces reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma[1].
MT 63-78 (0-50 μM; 30 minutes; LNCaP and PC3 cells) treatment shows a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. And also increases Thr172 phosphorylation on the AMPK α subunit[1].

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

MT 63-78 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP and PC3 cells
Concentration: 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM
Incubation Time: 4 days
Result: A dose-dependent decrease in cell number, concomitant to the activation of AMPK signaling was observed.

Cell Cycle Analysis[1]

Cell Line: LNCaP and CRPC cells
Concentration: 25 μM
Incubation Time: 24 hours
Result: Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models.

Apoptosis Analysis[1]

Cell Line: LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells
Concentration: 0 μM, 10 μM, 25 μM, 50 μM
Incubation Time: 24 hours
Result: Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma in all PCa cells.

Western Blot Analysis[1]

Cell Line: LNCaP and PC3 cells
Concentration: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM
Incubation Time: 30 minutes
Result: Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed.
In Vivo

MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth[1].

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

Animal Model: C57 BL/6 male mice bearing LNCaP tumors[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; daily; for 14 days
Result: Led to a 33% inhibition of tumor growth.
Molecular Weight

326.35

Formula

C21H14N2O2
CAS No.
Appearance

Solid

Color

Light yellow to brown

SMILES

N#CC1=CNC2=C1C=C(C3=CC=C(C4=C(O)C=CC=C4O)C=C3)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (383.02 mM; Need ultrasonic; 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 3.0642 mL 15.3210 mL 30.6419 mL
5 mM 0.6128 mL 3.0642 mL 6.1284 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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: ≥ 2.08 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0642 mL 15.3210 mL 30.6419 mL 76.6049 mL
5 mM 0.6128 mL 3.0642 mL 6.1284 mL 15.3210 mL
10 mM 0.3064 mL 1.5321 mL 3.0642 mL 7.6605 mL
15 mM 0.2043 mL 1.0214 mL 2.0428 mL 5.1070 mL
20 mM 0.1532 mL 0.7660 mL 1.5321 mL 3.8302 mL
25 mM 0.1226 mL 0.6128 mL 1.2257 mL 3.0642 mL
30 mM 0.1021 mL 0.5107 mL 1.0214 mL 2.5535 mL
40 mM 0.0766 mL 0.3830 mL 0.7660 mL 1.9151 mL
50 mM 0.0613 mL 0.3064 mL 0.6128 mL 1.5321 mL
60 mM 0.0511 mL 0.2553 mL 0.5107 mL 1.2767 mL
80 mM 0.0383 mL 0.1915 mL 0.3830 mL 0.9576 mL
100 mM 0.0306 mL 0.1532 mL 0.3064 mL 0.7660 mL
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MT 63-78 Related Classifications

Help & FAQs
  • 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:

MT 63-781179347-65-9AMPKmTORApoptosisAMP-activated protein kinaseMammalian target of RapamycinmTORC1directThr172dephosphorylationMcl-1BH3mitoticarrestp53RaptorlipogenesisantitumorInhibitorinhibitorinhibit

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