TH9028

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].

Product Specifications

CAS Number

2379556-15-5

UNSPSC

12352005

Target

Methylenetetrahydrofolate Dehydrogenase (MTHFD)

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/th9028.html

Smiles

NC(NC(N)=NC1=O)=C1NC(NC2=CN=C(C(N[C@H](C(O)=O)CCC3=NN=NN3)=O)C=C2)=O

Molecular Formula

C16H18N12O5

Molecular Weight

458.39

References & Citations

[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.|[2]Jha V, et al. Selectivity analysis of diaminopyrimidine-based inhibitors of MTHFD1, MTHFD2 and MTHFD2L[J]. Scientific Reports, 2024, 14 (1) : 21073.