PHGDH inhibitor D5-2

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Chemical Structure : PHGDH inhibitor D5-2

Catalog No.: PC-27040Not For Human Use, Lab Use Only.

PHGDH inhibitor D5-2 is a selective, covalent inhibitor of PHGDH (MST Kd=3.4 uM) engaging the interfacial Cys281, potently disrupts PHGDH dimerization and inhibits its enzymatic activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PHGDH inhibitor D5-2 is a selective, covalent inhibitor of PHGDH (MST Kd=3.4 uM) engaging the interfacial Cys281, potently disrupts PHGDH dimerization and inhibits its enzymatic activity.
D5-2 restores sensitivity to EGFR tyrosine kinase inhibitors in resistant lung adenocarcinoma cells in vitro, and exhibits antitumor efficacy in mouse xenograft models.

Physicochemical Properties

M.Wt	596.74
Formula	C32H40N10O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-2-((4-(2-(but-2-ynoyl)-2,8-diazaspiro[4.5]decan-8-yl)-6-(methylamino)-1,3,5-triazin-2-yl)amino)-3-(4-(6-(dimethylamino)pyridin-3-yl)phenyl)propanamide

References

1. Feng L, et al. J Med Chem. 2026 Jun 12. doi: 10.1021/acs.jmedchem.6c00456.

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