nudt5

TH5427 is a lead NUDT5 inhibitor(MG assay IC50 = 29 nM).

NUDT5/14 antagonist 1 (Compound 9) is a dual selective antagonist for nucleotide diphosphate kinases NUDT5 and NUDT14, exhibiting IC50 values of 0.27 and 0.16 μM, respectively. Additionally, NUDT5/14 antagonist 1 binds to Bruton's tyrosine kinase (BTK) with an IC50 of 0.377 μM.

TH287 is a potent inhibitor of MTH1 (NUDT1), less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.

DDD2 is a selective and efficient VHL-mediated PROTAC degrader specifically targeting NUDT5. It effectively induces substantial degradation of NUDT5. DDD2 consists of the warhead TH10184 and the VHL-recruiting ligand VH032, connected via a saturated aliphatic eight-carbon linker. DDD2 is applicable in cancer research, including studies on lymphocytic leukemia and osteosarcoma.

TH10184-octanedioic acid is a conjugate of the NUDT5 ligand and linker. It is utilized in the synthesis of DDD2, which is a PROTAC targeting degrader for NUDT5.

TH10184 is an inhibitor of NUDT5. It can be conjugated with VH032 and a linker to form a PROTAC-targeted degrader of NUDT5, known as DDD2.

TH5427 hydrochloride is a potent and selective inhibitor of NUDT5 with an IC50 of 29 nM. It demonstrates a remarkable 690-fold selectivity towards NUDT5 compared to MTH1. Moreover, TH5427 hydrochloride effectively inhibits progestin-dependent, PAR-derived nuclear ATP synthesis in breast cancer cells, thereby impeding chromatin remodeling, gene regulation, and ultimately suppressing proliferation.