Phosphoglycerate Dehydrogenase (PHGDH)

Phosphoglycerate dehydrogenase (PHGDH) is involved in the early steps of L-serine synthesis in animal cells. L-Serine is a pivotal amino acid since it serves as a precursor to a large number of essential metabolites besides D-serine, a major agonist of the N-methyl-D-aspartate (NMDA) receptor. PHGDH is the first and only rate-limiting enzyme in the de novo serine biosynthetic pathway and catalyzes the oxidation of 3-PG derived from glycolysis to 3-phosphohydroxypyruvate (3-PHP). Mutations in PHGDH gene have been found in a family with congenital microcephaly, psychomotor retardation and other symptoms. An increase in PGDH levels, due to overexpression, is also associated with a wide array of cancers. In culture, PGDH is required for tumor cell proliferation, but extracellular L-serine is not able to support cell proliferation. This has led to the hypothesis that the pathway is performing some function related to tumor growth other than supplying L-serine.

Phosphoglycerate Dehydrogenase (PHGDH) Related Products (19):

By Effects:	Inhibitors (9) Degrader (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-101966

NCT-503		99.69%
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC₅₀ of 2.5 µM.

HY-100012

CBR-5884		99.02%
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.

HY-141412

D-(-)-3-Phosphoglyceric acid disodium		99.43%
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.

HY-123269

PKUMDL-WQ-2101	Inhibitor	99.94%
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.

HY-126253

BI-4916		98.67%
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.

HY-179652

PHGDH-IN-6	Inhibitor
PHGDH-IN-6 (Compound L5) is a PHGDH allosteric inhibitor with an IC₅₀ of 2.5 μM. PHGDH-IN-6 can be used for studying diseases related to serine synthesis.

HY-117240

NCT-502		98.59%
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.

HY-121970

iGP-1	Inhibitor	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.

HY-126254

BI-4924		99.55%
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.

HY-121733

PHGDH-inactive		99.93%
PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503.

HY-148570

PHGDH-IN-3	Inhibitor	99.34%
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.

HY-123418

PKUMDL-WQ-2201	Inhibitor	98.45%
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.

HY-161456

PHGDH-IN-5	Inhibitor	98.12%
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.

HY-177742

LXH-3-71	Degrader
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.

HY-145860

PHGDH-IN-2
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.

HY-126278

Z1609609733	Inhibitor
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.

HY-125273

DNS-pE	Inhibitor
DNS-pE is a 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor with a K_i 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.

HY-101966R

NCT-503 (Standard)
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 phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC₅₀ of 2.5 µM.

HY-160252

PHGDH-IN-4	Inhibitor
PHGDH-IN-4 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-4 can be used for the research of cancer.

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