Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor
- 1
-
NCT-503
0 ImagesNCT-503 is a blood-brain barrier-permeable, non-competitive PHGDH inhibitor with an IC50 of 2.5 μM against human PHGDH. NCT-503 reduces glucose-derived serine production and the incorporation of one-carbon units into nucleotides without decreasing PHGDH protein expression. NCT-503 prevents high selenium-induced insulin resistance in mice by regulating blood glucose and insulin levels and improving glucose tolerance, and also inhibits the growth of tumors overexpressing PHGDH. NCT-503 can be used in research related to insulin resistance and breast cancer.
-
PKUMDL-WQ-2101
0 ImagesPKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity.
-
PHGDH-IN-7
0 ImagesCat. No.: HY-184449PHGDH-IN-7 is an orally active Cys281-targeted covalent noncompetitive PHGDH inhibitor with an enzymatic IC50 of 0.8 μM, MST Kd of 3.4 μM, and Ki of 2.82 μM. PHGDH-IN-7 disrupts PHGDH homodimer formation. PHGDH-IN-7 blocks cellular de novo serine synthesis. PHGDH-IN-7 elevates intracellular ROS levels and inhibits DNA replication. PHGDH-IN-7 resensitizes EGFR-TKI-resistant lung adenocarcinoma cells. PHGDH-IN-7 suppresses triple-negative breast tumor growth with no obvious systemic toxicity. PHGDH-IN-7 serves as a tool compound for PHGDH-dependent tumor research.
-
GDD-261
0 ImagesCat. No.: HY-184416GDD-261 is an orally active potent allosteric PHGDH inhibitor with IC50 of 61 nM and KD of 1.17 μM. GDD-261 potently suppresses de novo serine biosynthesis via blocking the rate-limiting catalytic activity of PHGDH, elevates intracellular reactive oxygen species (ROS) and γ-H2AX levels, and reduces the GSH/GSSG ratio to trigger tumor cell oxidative stress and DNA damage. GDD-261 mainly applies to research on Erlotinib (HY-50896)-resistant EGFR-mutant non-small cell lung cancer.
-
iGP-1
0 ImagesiGP-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.
-
PHGDH-IN-3
0 ImagesPHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.
-
PHGDH-IN-6
0 ImagesCat. No.: HY-179652PHGDH-IN-6 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 μM. PHGDH-IN-6 binds to the allosteric pocket of PHGDH, and its inhibitory activity is not affected by NAD+ concentration. PHGDH-IN-6 can be used in research related to cancer and Alzheimer's disease.
-
Z1609609733
0 ImagesCat. No.: HY-126278CAS No.: 2375374-15-3Z1609609733 (Compound 18) is a non-covalent 3-Phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 1.46 μM. Z1609609733 significantly inhibits serine synthesis and cancer metabolism with complete abrogation of cell proliferation.
-
DNS-pE
0 ImagesCat. No.: HY-125273CAS No.: 2196245-98-2DNS-pE is a 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor with a Ki of 7.4 μM. DNS-pE selectively and irreversibly covalently modifies endogenous PHGDH in live mammalian cells, its vinyl sulfone moiety acts as a fluorescence quencher that becomes highly fluorescent upon covalent modification of PHGDH. DNS-pE can be used as a fluorescent dye for live-cell imaging.
-
PHGDH-IN-4
0 ImagesCat. No.: HY-160252CAS No.: 2132969-16-3PHGDH-IN-4 is a potent 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor . PHGDH-IN-4 can be used for the research of cancer .
- 1
