Pro-GA
Based on 1 Customer Validation
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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- Purity: 97.86%
- CAS No.: 2222067-12-9
- 화학식: C12H19NO7
- 분자량:289.28
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:UMUC3, T24, RT112
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Concentration:50 μM, 80 μM (2-6 days); 0-180 μM (72 h)
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Incubation Time:2-6 days (dose-dependent growth inhibition); 72 h (IC50 determination)
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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.
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Cell Line:MCF7 human breast cancer cells
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Concentration:50, 75, 100 μM
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Incubation Time:0, 1, 2, 3, 4, 5 days
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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.
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Cell Line:MCF7 human breast cancer cells
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Concentration:50, 75 μM
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Incubation Time:72 h
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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.
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Cell Line:MCF7 human breast cancer cells
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Concentration:50 μM
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Incubation Time:72 h
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Result:Increased the protein expression of p21, p27, and p16 in MCF7 cells; this induction was suppressed by NAC cotreatment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB-17 severe combined immunodeficient (female, 14 weeks old, MCF7 human breast cancer cells inoculated into mammary fat pad)[2]
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Dosage:25 mg/kg
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Administration:i.p.; twice a week; 4 weeks
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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.
Chemical Information
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CAS No. 2222067-12-9
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Appearance Solid-Liquid Mixture
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분자량 289.28
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화학식 C12H19NO7
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Color Off-white to light yellow
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SMILES
O=C(OC)CCCC(N[C@@H](C)C(OCOC(C)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
용액&용해도
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Hanada E, et al. Pro-GA, a Novel Inhibitor of γ-Glutamylcyclotransferase, Suppresses Human Bladder Cancer Cell Growth. Anticancer Res. 2019;39(4):1893-1898. [Content Brief]
[2]. Ii H, et al. The γ-Glutamylcyclotransferase Inhibitor Pro-GA Induces an Antiproliferative Effect Through the Generation of Mitochondrial Reactive Oxygen Species. Anticancer Res. 2022;42(9):4311-4317. [Content Brief]
Complete Stock Solution Preparation Table
| 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 |
Pro-GA Related Classifications
HY-171030 Related Classifications
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