For research use only. Not for therapeutic Use.
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].
BI-4924 is a highly potent co-factor nicotinamide adenine dinucleotide (NADH/NAD+)-competitive PHGDH inhibitor. BI-4924 shows high selectivity against the majority of other dehydrogenase targets[1].
| Catalog Number | I018691 |
| CAS Number | 2244452-09-1 |
| Synonyms | 2-[4-[(1S)-1-[(4,5-dichloro-1,6-dimethylindole-2-carbonyl)amino]-2-hydroxyethyl]phenyl]sulfonylacetic acid |
| Molecular Formula | C21H20Cl2N2O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C21H20Cl2N2O6S/c1-11-7-16-14(20(23)19(11)22)8-17(25(16)2)21(29)24-15(9-26)12-3-5-13(6-4-12)32(30,31)10-18(27)28/h3-8,15,26H,9-10H2,1-2H3,(H,24,29)(H,27,28)/t15-/m1/s1 |
| InChIKey | CJEJFFCPVBZSIE-OAHLLOKOSA-N |
| SMILES | CC1=CC2=C(C=C(N2C)C(=O)NC(CO)C3=CC=C(C=C3)S(=O)(=O)CC(=O)O)C(=C1Cl)Cl |
| Reference | [1]. Weinstabl H, et al. Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis. J Med Chem. 2019 Jul 31. |
