27031-00-1
Chemical Structure
iGP-1
- CAS No.: 27031-00-1
- Formula:C17H15N3O3
- Molecular Weight:309.32
IUPAC Name: 4-((4-(1H-benzo[d]imidazol-2-yl)phenyl)amino)-4-oxobutanoic acid
InChIKey: ARVPDCQNTCJVSU-UHFFFAOYSA-N
SMILES: O=C(CCC(NC1=CC=C(C=C1)C2=NC3=CC=CC=C3N2)=O)O
Biological Activity: 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].
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iGP-1 | 99.43% | 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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- [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]
Keywords
