mth1

MTH1-IN-2 is an inhibitor of MutT homolog 1 (MTH1), with anti-tumor activity.

TH588 is nudix hydrolase family inhibitor that effectively and selectively engages and inhibits the MTH1(IC50: 5 nM) in cells.

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

TH287 is a selective MTH1 inhibitor(IC50 : 0.8 nM). It causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.

3-Isomangostin is a potent human aldose reductase inhibitor with an IC50 of 3.48 uM; it is also an acetylcholinesterase selective inhibitor. 3-Isomangostin has free radical scavenging activity; it shows antiplasmodial activity with IC50 values in the rang

(S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

MTH1 ligand 1 functions as a target protein ligand for MTH1, and is utilized in the synthesis of PROTACaTAG 2139.

MTH1 degrader-1 is an inhibitor of MTH1 aTAG and serves as a ligand for target proteins in PROTAC applications. It is used in the synthesis of PROTAC aTAG 4531.

MTH1 activator-1 is an MTH1 activator that enhances endogenous MTH1 activity and significantly reduces 8-oxo-dG levels in cellular DNA. It is useful for investigating the upregulation of oxidative damage repair in nucleotide pools and examining biological effects, as well as for studies aiming to delay or prevent tumorigenesis.

CMP-5 is a PRMT5 inhibitor with antiviral activity, inhibits PRMT5 methyltransferase activity, and can be used in the study of SARS virus infection.

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

CMP-5 hydrochloride is a potent and selective PRMT5 inhibitor, while displays no activity against PRMT1/4/7 enzymes. It selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations.

FKBP12PROTACFM4 is a PROTAC degrader targeting MTH1, with a degradation efficiency (Dmax) greater than 90%.

8-Oxo-dATP can be hydrolyzed to its monophosphate form by the oxidation of purine nucleoside triphosphate MTH1, preventing erroneous incorporation during DNA replication or transcription.

TH086 is a MTH1 inhibitor.

NPD7155 is a competitive inhibitor of MTH1.

NPD9948 is a competitive inhibitor of MTH1.

Degrader of MTH1 fusion proteins for use within the aTAG system. Comprises a ligand selective for MTH1, a linker and the cereblon-binding ligand Thalidomide . Induces highly potent and selective degradation of fusion proteins after a 4 h incubation (DC50 = 0.27 nM; Dmax = 92.1%). Cell-permeable. Suitable for in vitro and in vivo applications. Mouse DMPK properties are provided in the supplementary file (see below). (MTH1 can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in - see protocol for more information.) 0

Degrader of MTH1 fusion proteins for use within the aTAG system. Comprises a ligand selective for MTH1, a linker and the cereblon-binding ligand Thalidomide . Induces highly potent and selective degradation of fusion proteins after a 4 h incubation (DC50 = 0.34 nM; Dmax = 93.14%). Cell-permeable. Suitable for in vitro and in vivo applications. Mouse DMPK properties are provided in the supplementary file (see below). (MTH1 can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in - see protocol for more information.) 0

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.

TH588 hydrochloride, a first-in-class inhibitor of the nudix hydrolase family, selectively and effectively binds to and inhibits MTH1 with an IC50 value of 5 nM.

BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1. Despite superior cellular target engagement and pharmacokinetic properties, inhibition of MTH1 with BAY-707 resulted in a clear lack of in vitro or in vivo anticancer efficacy either in mono- or in combination therapies.

IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes.

Isoguanosine-5'-O-triphosphate, an isomer of guanosine 5'-triphosphate (GTP) and a phosphorylated derivative of crotonoside, does not promote microtubule assembly like GTP. At a concentration of 2 mM, it hampers transcription and triggers T to C mutations in reverse transcriptase assays. This compound aids in assessing the substrate specificity of both phosphofructokinase and mutT homolog 1 (MTH1).