2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Phosphoglycerate Dehydrogenase (PHGDH) Reactive Oxygen Species (ROS) HIF/HIF Prolyl-Hydroxylase
  4. iGP-1

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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iGP-1

iGP-1 Chemical Structure

CAS No. : 27031-00-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

iGP-1 Related Antibodies

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Description

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[1][2][3].

IC50 & Target

HIF-1α

 

In Vitro

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.

iGP-1 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: PC-3 androgen receptor-negative prostate cancer cells
Concentration: 100 μM, 300 μM, 400 μM
Incubation Time: 96 h
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.

Cell Proliferation Assay[2]

Cell Line: DU145 androgen receptor-negative prostate cancer cells
Concentration: 300 μM
Incubation Time: 96 h
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.
Molecular Weight

309.32

Formula

C17H15N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCC(NC1=CC=C(C=C1)C2=NC3=CC=CC=C3N2)=O)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2329 mL 16.1645 mL 32.3290 mL
5 mM 0.6466 mL 3.2329 mL 6.4658 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (8.08 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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(per animal)

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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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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).
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

Purity: 99.43%

SDS (392 KB)

COA (246 KB) HNMR (134 KB) RP-HPLC (248 KB) LCMS (386 KB)

Handling Instructions (2659 KB)
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. 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
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iGP-1 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:

iGP-127031-00-1iGP1iGP 1Phosphoglycerate Dehydrogenase (PHGDH)Reactive Oxygen Species (ROS)HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHSTHdhQ7 cellsStaphylococcus aureusmitochondrial sn-glycerol 3-phosphate dehydrogenaseprostate cancerDU145 cellPC-3 cellglycerophosphate shuttleneutrophilcytosolic GPDHmGPDHInhibitorinhibitorinhibit

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