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18

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12122	MTH1-IN-2	MTH1	DNA Damage/DNA Repair
	MTH1-IN-2 is an inhibitor of MutT homolog 1 (MTH1), with anti-tumor activity.
T2037	TH588	DNA/RNA Synthesis; MTH1	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	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。
T2069	TH287 TH287 hydrochloride	DNA/RNA Synthesis; MTH1	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	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。
T6357	(S)-crizotinib ent-crizotinib	Apoptosis; DNA/RNA Synthesis; MTH1	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	(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。
T2069L	TH287 hydrochloride	DNA/RNA Synthesis; MTH1	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	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。
T28194	NPD9948 NPD-9948,NPD 9948
	NPD9948 is a competitive inhibitor of MTH1.
T14509	BAY-707	Others	Others
	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].
T69776	BAY-707 acetate
	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.
T70091	IACS-4759
	IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes.
T28192	NPD7155 NPD-7155,NPD 7155
	NPD7155 is a competitive inhibitor of MTH1.
T24875	TH086 TH 086,TH-086
	TH086 is a MTH1 inhibitor.
T60984	TH588 hydrochloride
	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。
T35475	aTAG 4531
	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 genom...
T35474	aTAG 2139
	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...
T83818	Isoguanosine-5'-O-triphosphate sodium 2-Hydroxyadenosine 5’-triphosphate,2-hydroxy ATP,isoGTP
	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。
T39785	TH5427 hydrochloride
	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.
T10850	CMP-5	Others	Others
	CMP-5 是一种有效的、具有选择性的小分子 PRMT5 抑制剂。CMP-5可阻断EBV 驱动的B 淋巴细胞转化和存活，对 PRMT1，PRMT4 和 PRMT7 酶不显示此活性。CMP-5 在组蛋白的准备过程中，抑制 PRMT5 甲基转移酶活性，抑制miR96启动子上PRMT5/p65/HDAC3复合物的募集。
T19243	CMP-5 hydrochloride	Others	Others
	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.

化合物

Cat.No: T12122

Target: MTH1

Cat.No: T2037

Target: DNA/RNA Synthesis, MTH1

Cat.No: T2069

Synonym: TH287 hydrochloride

Target: DNA/RNA Synthesis, MTH1

Cat.No: T6357

Synonym: ent-crizotinib

Target: Apoptosis, DNA/RNA Synthesis, MTH1

TH287 hydrochloride

Cat.No: T2069L

Target: DNA/RNA Synthesis, MTH1

Cat.No: T28194

Synonym: NPD-9948,NPD 9948

Cat.No: T14509

Target: Others

BAY-707 acetate

Cat.No: T69776

Cat.No: T70091

Cat.No: T28192

Synonym: NPD-7155,NPD 7155

Cat.No: T24875

Synonym: TH 086,TH-086

TH588 hydrochloride

Cat.No: T60984

Cat.No: T35475

Cat.No: T35474

Isoguanosine-5'-O-triphosphate sodium

Cat.No: T83818

Synonym: 2-Hydroxyadenosine 5’-triphosphate,2-hydroxy ATP,isoGTP

TH5427 hydrochloride

Cat.No: T39785

Cat.No: T10850

Target: Others

CMP-5 hydrochloride

Cat.No: T19243

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T2S1635	3-Isomangostin	MTH1	DNA Damage/DNA Repair
	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。

天然产物

Cat.No: T2S1635

Target: MTH1

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