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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.
| Molecular Weight | 499.36 |
| CAS Number | 2244452-09-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PHGDH Products |
|---|
| PKUMDL-WQ-2101
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. |
| PHGDH-inactive
PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503. |
| NCT-502
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. |
| BI-4916
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD+-competitive PHGDH inhibitor. |
| NCT-503
NCT-503 is an inhibitor of phosphoglycerate dehydrogenase (PHGDH), which catalyzes the first, rate-limiting step of glucose-derived serine synthesis. |
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