| Identification | Back Directory | [Name]
Glycine, N-[[5-[[[(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)amino]carbonyl]amino]-2-pyridinyl]carbonyl]-2-[2-(2H-tetrazol-5-yl)ethyl]-, (2S)- | [CAS]
2379556-15-5 | [Synonyms]
TH9028
Glycine, N-[[5-[[[(2,4-diamino-1,6-dihydro-6-oxo-5-pyrimidinyl)amino]carbonyl]amino]-2-pyridinyl]carbonyl]-2-[2-(2H-tetrazol-5-yl)ethyl]-, (2S)- | [Molecular Formula]
C16H18N12O5 | [MOL File]
2379556-15-5.mol | [Molecular Weight]
458.39 |
| Hazard Information | Back Directory | [Uses]
TH9028 is an inhibitor of MTHFD2 (IC50 = 11 nM) with IC50 values against hMTHFD2, MTHFD2L, and MTHFD1 being 7.97 nM, 27 nM, and 0.5 nM, respectively. TH9028 also exhibits anti-cancer cell proliferation activity[1][2]. | [IC 50]
MTHFD2: 11 nM (IC50); hMTHFD2: 7.97 nM (IC50); MTHFD2L: 27 nM (IC50); MTHFD1: 0.5 nM (IC50) | [References]
[1] Bonagas N, et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress[J]. Nature cancer, 2022, 3(2): 156-172. DOI:10.1038/s43018-022-00331-y
[2] Jha V, et al. Selectivity analysis of diaminopyrimidine-based inhibitors of MTHFD1, MTHFD2 and MTHFD2L[J]. Scientific Reports, 2024, 14(1): 21073. DOI:10.1038/s41598-024-71879-1 |
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