1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Dehydrogenase (PHGDH)

Phosphoglycerate Dehydrogenase (PHGDH) (磷酸甘油酸脱氢酶)

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) 相关产品 (11):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101966
    NCT-503 99.85%
    NCT-503磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,IC50 值为2.5 µM。
    NCT-503
  • HY-100012
    CBR-5884 99.02%
    CBR-5884 是一种有效,选择性的磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,IC50 为 33 μM。 CBR-5884 抑制癌细胞中的丝氨酸合成,并且对具有高丝氨酸生物合成活性的癌细胞系具有选择性毒性。 CBR-5884 选择性地抑制黑素瘤和乳腺癌细胞系的增殖。
    CBR-5884
  • HY-117240
    NCT-502 99.18%
    NCT-502 是一种磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,对 PHGDH 依赖性癌细胞具有细胞毒性,减少葡萄糖衍生的丝氨酸的产生,对 PHGDH 的 IC50 值为 3.7 μM。
    NCT-502
  • HY-126253
    BI-4916 98.55%
    BI-4916 是 BI-4924 的前体。BI-4924 是一种 NADH/NAD+- 竞争性的磷酸甘油酸脱氢酶 (PHGDH) 抑制剂。 。
    BI-4916
  • HY-126254
    BI-4924 99.55%
    BI-4924 是一种亲脂性,与血浆蛋白高度结合的选择性磷酸甘油酸脱氢酶 (PHGDH) 抑制剂 (IC50=3 nM),具有优异的微粒体和肝细胞稳定性。胞内捕获 BI-4924 可破坏丝氨酸生物合成,作用 72 小时的 IC50 为 2200 nM。
    BI-4924
  • HY-121733
    PHGDH-inactive 99.72%
    PHGDH-inactive 对 PHGDH 无活性(IC50>57 μM),可作为 NCT-502 和 NCT-503 的阴性对照。
    PHGDH-inactive
  • HY-123269
    PKUMDL-WQ-2101 Inhibitor 99.85%
    PKUMDL-WQ-2101 是一种非 NAD+ 竞争性变构磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,IC50 为 34.8 μM。PKUMDL-WQ-2101 具有抗肿瘤活性。
    PKUMDL-WQ-2101
  • HY-148570
    PHGDH-IN-3 Inhibitor 98.99%
    PHGDH-IN-3 是一种磷酸甘油酸脱氢酶 (PHGDH) 抑制剂,具有口服活性。PHGDH-IN-3 抑制 PHGDH,IC50 值为 2.8 μM。PHGDH-IN-3 可用于癌症的研究。
    PHGDH-IN-3
  • HY-123418
    PKUMDL-WQ-2201 Inhibitor 98.72%
    PKUMDL-WQ-2201 是一种 PHGDH 非 NAD+ 竞争变构抑制剂 (IC50=35.7 μM)。PKUMDL-WQ-2201 对 PHGDH 突变体的 IC50 分别为 69 μM (T59A) 和300 μM (T56AK57A)。PKUMDL-WQ-2201 抑制癌细胞中丝氨酸的从头合成,并减少肿瘤生长。
    PKUMDL-WQ-2201
  • HY-145860
    PHGDH-IN-2
    PHGDH-IN-2 是一种有效的 NAD+ 竞争性 PHGDH 抑制剂,其IC50 值为 5.2 µM。PHGDH-IN-2 抑制 MDA-MB-468 细胞中的丝氨酸合成途径。PHGDH-IN-2 抑制 PHGDH 依赖性癌细胞的生长。
    PHGDH-IN-2
  • HY-160252
    PHGDH-IN-4 Inhibitor
    PHGDH-IN-4 是一种磷酸甘油酸脱氢酶 (PHGDH) 抑制剂。PHGDH-IN-4 可用于癌症研究。
    PHGDH-IN-4