iGP-1
Based on 1 Customer Validation
iGP-1 is a cell-permeable, selective mixed inhibitor of mitochondrial sn-glycerol-3-phosphate dehydrogenase (mGPDH), with IC50s of 6.3 μM and 13.6 μM for rat mGPDH activity and H2O2 production, respectively. iGP-1 specifically blocks the mitochondrial component of the glycerophosphate shuttle without affecting cytosolic GPDH. iGP-1 not only inhibits cell proliferation and glutaminolysis, and enhances glycolysis, but also significantly alters key cellular physiological processes such as apoptosis, ROS production, HIF-1α stability and mitochondrial membrane potential. iGP-1 remains active in neutrophil cultures under both normoxic and hypoxic conditions, and serves as an ideal probe for glycerol-3-phosphate metabolic mechanisms. iGP-1 has been applied to studies on prostate cancer and related metabolic pathways.
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- Pureza: 99.43%
- No. CAS: 27031-00-1
- Fòrmula: C17H15N3O3
- Peso molecular:309.32
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Help & FAQs
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Actividad biológica
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HIF-1α |
iGP-1 (0.1-80 μM) potently and selectively inhibits mGPDH-mediated H2O2 production in isolated rat skeletal muscle mitochondria, with an IC50 of 8 μM, and exhibits only weak off-target effects at concentrations above 10 μM[1].
iGP-1 (100 μM) can readily cross cell membranes and enter the cytoplasmic matrix and acidic compartments of STHdhQ7 cells[1].
iGP-1 (100-400 μM; 96 h) inhibits the proliferation of pyruvate-starved PC-3 cells by approximately 40% in low-pyruvate medium; in high-pyruvate medium, this inhibitory effect weakens to approximately 20% at a concentration of 300 μM, with increased glycolytic flux, reduced glutamate production, and no changes in the conversion rates of pyruvate, glutamine, alanine or serine[2].
iGP-1 (10-1000 μM) concentration-dependently reduces the mitochondrial membrane potential of human primary peripheral blood neutrophils under both normoxic and hypoxic conditions[3].
iGP-1 (1-1000 μM; 4 h) reduces HIF-1α protein expression in hypoxic human primary peripheral blood neutrophils in a concentration-dependent manner[3].
iGP-1 (10-1000 μM; 1 h) reduces mitochondrial ROS levels in primary human peripheral blood neutrophils after 1 hour of treatment in a concentration-dependent manner under both normoxic and hypoxic conditions[3].
iGP-1 (1-1000 μM; 20 h) induces apoptosis in human primary peripheral blood neutrophils in a concentration-dependent manner, and its pro-apoptotic effect is stronger after 20 h of treatment under hypoxic conditions[3].
iGP-1 (100-1000 μM; 4 h) concentration-dependently inhibits myeloperoxidase release (degranulation) in human primary peripheral blood neutrophils under both normoxic and hypoxic conditions, following 4 hours of pre-stimulation treatment[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3 androgen receptor-negative prostate cancer cells
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Concentration:100 μM, 300 μM, 400 μM
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Incubation Time:96 h
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Result:Induced an approximately 40% inhibition of PC-3 cell proliferation in pyruvate-low medium.
Induced only 20% inhibition of PC-3 cell proliferation at 300 μM in pyruvate-high medium.
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Cell Line:DU145 androgen receptor-negative prostate cancer cells
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Concentration:300 μM
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Incubation Time:96 h
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Result:Induced a 15% inhibition of DU145 cell proliferation in pyruvate-low medium.
Induced an 8% inhibition of DU145 cell proliferation in pyruvate-high medium.
Chemical Information
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No. CAS 27031-00-1
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Appearance Solid
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Peso molecular 309.32
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Fòrmula C17H15N3O3
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Color White to off-white
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SMILES
O=C(CCC(NC1=CC=C(C=C1)C2=NC3=CC=CC=C3N2)=O)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (323.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.08 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.
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Orr AL, et al. Novel inhibitors of mitochondrial sn-glycerol 3-phosphate dehydrogenase. PLoS One. 2014;9(2):e89938. Published 2014 Feb 24. [Content Brief]
[2]. Di Paola FJ, et al. Impact of mtG3PDH inhibitors on proliferation and metabolism of androgen receptor-negative prostate cancer cells: Role of extracellular pyruvate. PLoS One. 2025;20(6):e0325509. Published 2025 Jun 9. [Content Brief]
[3]. Willson JA, et al. Neutrophil HIF-1α stabilization is augmented by mitochondrial ROS produced via the glycerol 3-phosphate shuttle. Blood. 2022 Jan 13;139(2):281-286. [Content Brief]
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. 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 | 3.2329 mL | 16.1645 mL | 32.3290 mL | 80.8224 mL |
| 5 mM | 0.6466 mL | 3.2329 mL | 6.4658 mL | 16.1645 mL | |
| 10 mM | 0.3233 mL | 1.6164 mL | 3.2329 mL | 8.0822 mL | |
| 15 mM | 0.2155 mL | 1.0776 mL | 2.1553 mL | 5.3882 mL | |
| 20 mM | 0.1616 mL | 0.8082 mL | 1.6164 mL | 4.0411 mL | |
| 25 mM | 0.1293 mL | 0.6466 mL | 1.2932 mL | 3.2329 mL | |
| 30 mM | 0.1078 mL | 0.5388 mL | 1.0776 mL | 2.6941 mL | |
| 40 mM | 0.0808 mL | 0.4041 mL | 0.8082 mL | 2.0206 mL | |
| 50 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.6164 mL | |
| 60 mM | 0.0539 mL | 0.2694 mL | 0.5388 mL | 1.3470 mL | |
| 80 mM | 0.0404 mL | 0.2021 mL | 0.4041 mL | 1.0103 mL | |
| 100 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL |
iGP-1 Related Classifications
HY-121970 Related Classifications
Powered by Bioz
- iGP-1
- 27031-00-1
- iGP1
- iGP 1
- Phosphoglycerate Dehydrogenase (PHGDH)
- Reactive Oxygen Species (ROS)
- HIF/HIF Prolyl-Hydroxylase
- STHdhQ7 cells
- Staphylococcus aureus
- mitochondrial sn-glycerol 3-phosphate dehydrogenase
- prostate cancer
- DU145 cell
- PC-3 cell
- glycerophosphate shuttle
- neutrophil
- cytosolic GPDH
- mGPDH
- Inhibitor
- inhibitor
- inhibit