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Cat. No. | Product Name | Target | Signaling Pathways |
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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 |
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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 |
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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 |
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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
|
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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 1(MTH1)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. |
Cat. No. | Product Name | Target | Signaling Pathways |
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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。 |
Cat. No. | Product Name | Species | Expression System |
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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... |