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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
19 Results for "
PHGDH inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "PHGDH inhibitor" in MCE Product Catalog:
33
33 Publications Verification
Research Areas:
NCT-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 .
21
21 Cited Publications
Research Areas:
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis .
7
7 Cited Publications
Research Areas:
BI-4916 is a proagent of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor. BI-4916 inhibits cancer cell migration. BI-4916 can be used for cancer, inflammation and infection study .
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6 Cited Publications
Research Areas:
NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH .
1
1 Cited Publications
Synonyms: 3-Phospho-D-glyceric acid disodium
Research Areas:
D-(-)-3-Phosphoglyceric acid (3-Phospho-D-glyceric acid) disodium is an important intermediate in the enzyme-catalyzed glycolysis process. D-(-)-3-Phosphoglyceric acid disodium competitively inhibits yeast enolase (enolase). D-(-)-3-Phosphoglyceric acid disodium can regulate the activity of phosphoglycerate dehydrogenase (PHGDH) to modulate p53 protein and apoptosis .
1
1 Cited Publications
Research Areas:
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h .
1
1 Cited Publications
Research Areas:
PHGDH-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 .
Research Areas:
PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth .
Research Areas:
PKUMDL-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 .
Cat. No.: HY-161456
CAS No.: 17402-86-7
Research Areas:
PHGDH-IN-5 (Compound B12) is a covalen inhibitor of PHGDH with an IC50 value of 0.29 μM. PHGDH-IN-5 can inhibit cell proliferation in cancer cell lines overexpressing PHGDH. PHGDH-IN-5 can reduce the production of serine derived from glucose in MDA-MB-468 cells .
Cat. No.: HY-125273
CAS No.: 2196245-98-2
Research Areas:
DNS-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 .
Cat. No.: HY-126278
CAS No.: 2375374-15-3
Research Areas:
Z1609609733 (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 .
Cat. No.: HY-145860
Research Areas:
PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
Cat. No.: HY-160252
CAS No.: 2132969-16-3
Research Areas:
PHGDH-IN-4 is a potent 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor . PHGDH-IN-4 can be used for the research of cancer .
Cat. No.: HY-177742
CAS No.: 2251753-65-6
Research Areas:
LXH-3-71 is a PHGDH degrader. LXH-3-71 acts as a molecular glue to enhance the interaction of the PHGDH-DDB1-CRL E3 ligase complex, triggering ubiquitination and proteasomal degradation of PHGDH. LXH-3-71 regulates the stemness of colorectal cancer cells and inhibits tumor proliferation and colony formation. LXH-3-71 can be used in the research of colorectal cancer .
Cat. No.: HY-184449
Research Areas:
PHGDH-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 .
Cat. No.: HY-179652
Research Areas:
PHGDH-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 .
Cat. No.: HY-101966R
CAS No.: 1916571-90-8
Research Areas:
NCT-503 (Standard) is the analytical standard of NCT-503 (HY-101966). This product is intended for research and analytical applications. NCT-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 .
Cat. No.: HY-184416
Research Areas:
GDD-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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
