1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  2. Reactive Oxygen Species (ROS)
  3. Pro-GA

Pro-GA is a γ-glutamyl cyclotransferase (GGCT) inhibitor. Pro-GA inhibits the enzymatic activity of GGCT, disrupts glutathione homeostasis, induces the production of mitochondrial ROS, and upregulates the expression of p21, p27 and p16 in cells. Pro-GA inhibits the growth of cancer cells, induces cell cycle arrest and cellular senescence. Pro-GA exerts anti-tumor effects in breast cancer xenograft mouse models. Pro-GA can be used in research related to bladder cancer and breast cancer.

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Pro-GA

Pro-GA Chemical Structure

CAS No. : 2222067-12-9

Size Price Stock Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Description

Pro-GA is a γ-glutamyl cyclotransferase (GGCT) inhibitor. Pro-GA inhibits the enzymatic activity of GGCT, disrupts glutathione homeostasis, induces the production of mitochondrial ROS, and upregulates the expression of p21, p27 and p16 in cells. Pro-GA inhibits the growth of cancer cells, induces cell cycle arrest and cellular senescence. Pro-GA exerts anti-tumor effects in breast cancer xenograft mouse models. Pro-GA can be used in research related to bladder cancer and breast cancer[1][2].

In Vitro

Pro-GA (0-180 μM; 0-6 days) inhibits the growth of human bladder cancer UMUC3, T24 and RT112 cells in a dose-dependent manner, with IC50 values of 73.9 μM, 57.0 μM and 58.5 μM, respectively[1].
Pro-GA (100 μM) significantly enhances the anti-tumor effect of Mitomycin C (HY-13316) on RT112, UMUC3 and T24 human bladder cancer cells[1].
Pro-GA (50-100 μM; 1-5 days) inhibits the viability of human breast cancer MCF7 cells in a dose-dependent manner, suppresses DNA synthesis in cells, and reduces the number of viable cells[2].
Pro-GA (50 μM; 72 h) upregulates the expression of cyclin-dependent kinase inhibitors p21, p27 and p16 in human breast cancer MCF7 cells[2].
Pro-GA (75 μM; 72 h) increases the level of mitochondrial reactive oxygen species in human breast cancer MCF7 cells[2].
Pro-GA (50-75 μM; 96 h) induces cellular senescence in human breast cancer MCF7 cells[2].

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

Cell Proliferation Assay[1]

Cell Line: UMUC3, T24, RT112
Concentration: 50 μM, 80 μM (2-6 days); 0-180 μM (72 h)
Incubation Time: 2-6 days (dose-dependent growth inhibition); 72 h (IC50 determination)
Result: Reduced the viability of all three bladder cancer cell lines in a dose-dependent manner.
Reached IC50 values of 73.9 μM for RT112, 57.0 μM for T24, and 58.5 μM for UMUC3.

Cell Viability Assay[2]

Cell Line: MCF7 human breast cancer cells
Concentration: 50, 75, 100 μM
Incubation Time: 0, 1, 2, 3, 4, 5 days
Result: Inhibited MCF7 cell growth in a dose-dependent manner, with significant reductions in relative cell viability observed at all tested concentrations and time points compared to vehicle control.

Cell Proliferation Assay[2]

Cell Line: MCF7 human breast cancer cells
Concentration: 50, 75 μM
Incubation Time: 72 h
Result: Significantly reduced the percentage of MCF7 cells undergoing active DNA synthesis, with 50 μM causing a significant reduction and 75 μM causing a more pronounced significant reduction compared to vehicle control.

Western Blot Analysis[2]

Cell Line: MCF7 human breast cancer cells
Concentration: 50 μM
Incubation Time: 72 h
Result: Increased the protein expression of p21, p27, and p16 in MCF7 cells; this induction was suppressed by NAC cotreatment.
In Vivo

pro-GA (25 mg/kg; i.p.; twice weekly for 4 consecutive weeks) significantly inhibits the growth of MCF7 breast cancer xenografts in immunodeficient mice[2].

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

Animal Model: CB-17 severe combined immunodeficient (female, 14 weeks old, MCF7 human breast cancer cells inoculated into mammary fat pad)[2]
Dosage: 25 mg/kg
Administration: i.p.; twice a week; 4 weeks
Result: Significantly inhibited MCF7 xenograft tumor growth relative to controls, with statistically significant reduction in relative tumor volume and tumor weight after 4 weeks of treatment.
Showed no obvious change in mouse body weight during the treatment period, indicating no overt toxicity.
Molecular Weight

289.28

Formula

C12H19NO7

CAS No.
Appearance

Solid-Liquid Mixture

Color

Off-white to light yellow

SMILES

O=C(OC)CCCC(N[C@@H](C)C(OCOC(C)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (172.84 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 3.4569 mL 17.2843 mL 34.5686 mL
5 mM 0.6914 mL 3.4569 mL 6.9137 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 (sealed storage, away from moisture and 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.64 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
%
Tween-80 +
%
Saline
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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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 3.4569 mL 17.2843 mL 34.5686 mL 86.4215 mL
5 mM 0.6914 mL 3.4569 mL 6.9137 mL 17.2843 mL
10 mM 0.3457 mL 1.7284 mL 3.4569 mL 8.6421 mL
15 mM 0.2305 mL 1.1523 mL 2.3046 mL 5.7614 mL
20 mM 0.1728 mL 0.8642 mL 1.7284 mL 4.3211 mL
25 mM 0.1383 mL 0.6914 mL 1.3827 mL 3.4569 mL
30 mM 0.1152 mL 0.5761 mL 1.1523 mL 2.8807 mL
40 mM 0.0864 mL 0.4321 mL 0.8642 mL 2.1605 mL
50 mM 0.0691 mL 0.3457 mL 0.6914 mL 1.7284 mL
60 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4404 mL
80 mM 0.0432 mL 0.2161 mL 0.4321 mL 1.0803 mL
100 mM 0.0346 mL 0.1728 mL 0.3457 mL 0.8642 mL
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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.

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Pro-GA
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