mth1

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

TH588 是 nudix 水解酶家族抑制剂，可有效和选择性地参与和抑制细胞中的 MTH1，IC50值 5 nM。

TH287 是一种选择性的MTH1抑制剂，对 MTH1 具有高度选择性，可用于治疗癌症的研究。

3-Isomangostin 可从莽吉柿壳中提取的一种天然产物，是一种乙酰胆碱酯酶选择性抑制剂，也是一种有效的人醛糖还原酶抑制剂，IC50 为 3.48 uM。它抑制 MutT 同源物 1 (MTH1)，IC50 为 52 nM。它具有清除自由基、抗疟原虫和抗癌的活性。

(S)-crizotinib (ent-crizotinib) 是一种选择性MTH1(mutT 同源物)抑制剂，IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态，诱导 DNA 单链断裂的增加，激活人结肠癌细胞的 DNA 修复，在动物模型中抑制肿瘤生长。

TH287 hydrochloride 是一种选择性MTH1抑制剂，IC50值为 0.8 nM。它可用于治疗癌症的研究。

MTH1 ligand 1 为特定靶点MTH1的配体，适用于PROTACaTAG 2139的合成。

MTH1 degrader-1 是MTH1 aTAG抑制剂，也是PROTAC靶蛋白配体 (Ligand for Target Protein for PROTAC)，可用于合成PROTAC aTAG 4531。

MTH1 activator-1 是一种MTH1激活剂，能够提升内源性MTH1的活性，同时显著降低细胞DNA中的8-oxo-dG水平。此化合物适用于研究核苷酸池中氧化损伤修复的上调效应，以及用于延迟或减少肿瘤发生的实验。

CMP-5 是一种具有选择性的 PRMT5 抑制剂，是刺突蛋白、神经纤毛蛋白受体和 ACE2 的强结合剂,抑制 PRMT5 甲基转移酶活性。CMP-5 具有抗病毒活性，可用于研究SARS病毒感染。

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.

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 hydrochlorid 是创新的 nudix 水解酶家族抑制剂，可选择性的高效结合并抑制MTH1 (NUDT1)，IC50值为 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是guanosine 5'-triphosphate（GTP）的一个异构体且是crotonoside的磷酸化形式。与GTP不同，Isoguanosine-5'-O-triphosphate不促进微管组装。在逆转录酶实验中，Isoguanosine-5'-O-triphosphate（2 mM）能抑制转录并诱导T到C的突变。它已被用于确定phosphofructokinase和mutT homolog 1（MTH1）的底物特异性。