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Targets Recommended: MTH1 MTH1

18

抑制剂 & 化合物

1

天然产物

1

重组蛋白

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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].
T28192 NPD7155

NPD-7155,NPD 7155

NPD7155 is a competitive inhibitor of MTH1.
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.
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...
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.
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 1MTH1)的底物特异性。
T10850 CMP-5

Antiviral; Histone Methyltransferase Chromatin/Epigenetic; Immunology/Inflammation
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。
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

MTH1-IN-2
Cat.No: T12122
Synonym:
Target: MTH1
TH588
Cat.No: T2037
Synonym:
Target: DNA/RNA Synthesis, MTH1
TH287
Cat.No: T2069
Synonym: TH287 hydrochloride
Target: DNA/RNA Synthesis, MTH1
(S)-crizotinib
Cat.No: T6357
Synonym: ent-crizotinib
Target: Apoptosis, DNA/RNA Synthesis, MTH1
TH287 hydrochloride
Cat.No: T2069L
Synonym:
Target: DNA/RNA Synthesis, MTH1
NPD9948
Cat.No: T28194
Synonym: NPD-9948,NPD 9948
Target:
BAY-707
Cat.No: T14509
Synonym:
Target: Others
NPD7155
Cat.No: T28192
Synonym: NPD-7155,NPD 7155
Target:
BAY-707 acetate
Cat.No: T69776
Synonym:
Target:
IACS-4759
Cat.No: T70091
Synonym:
Target:
TH086
Cat.No: T24875
Synonym: TH 086,TH-086
Target:
TH588 hydrochloride
Cat.No: T60984
Synonym:
Target:
aTAG 4531
Cat.No: T35475
Synonym:
Target:
aTAG 2139
Cat.No: T35474
Synonym:
Target:
TH5427 hydrochloride
Cat.No: T39785
Synonym:
Target:
Isoguanosine-5'-O-triphosphate sodium
Cat.No: T83818
Synonym: 2-Hydroxyadenosine 5’-triphosphate,2-hydroxy ATP,isoGTP
Target:
CMP-5
Cat.No: T10850
Synonym:
Target: Antiviral, Histone Methyltransferase
CMP-5 hydrochloride
Cat.No: T19243
Synonym:
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

3-Isomangostin
Cat.No: T2S1635
Synonym:
Target: MTH1
Cat. No. Product Name Species Expression System
TMPY-00116 MTH1 Protein, Human, Recombinant (His)

MTH1,nudix (nucleoside diphosphate linked ...

Human E. coli
NUDT1 (Nudix Hydrolase 1) is a Protein Coding gene. The protein encoded by this gene is an enzyme that hydrolyzes oxidized purine nucleoside triphosphates to monophosphates, thereby preventing misincorporation. The NUDT1 protein is localized mainly in the cytoplasm, with some in the mitochondria, suggesting that it is involved in the sanitization of nucleotide pools both for nuclear and mitochondrial genomes. Cancers can survive the oxidative conditions by upregulating nucleoside diphosphate lin...

重组蛋白

MTH1 Protein, Human, Recombinant (His)
Cat.No: TMPY-00116
Species: Human
Expression System: E. coli
TargetMol Loading
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