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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
33 Results for "
MTH1
" in MedChemExpress (MCE) Product Catalog:
Products (33)
33 Results for "MTH1" in MCE Product Catalog:
3
3 Cited Publications
Target:
Research Areas:
(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models [1].
3
3 Cited Publications
Cat. No.: HY-16965
CAS No.: 1609960-30-6
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TH287 is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 could act as a chemotherapeutic agent for cancer research [1].
2
2 Cited Publications
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TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
Cat. No.: HY-N6845
CAS No.: 19275-46-8
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Cat. No.: HY-171230
CAS No.: 2803422-60-6
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MTH1 activator-1 is an MTH1 activator that enhances endogenous MTH1 activity and significantly reduces 8-oxo-dG levels in cellular DNA. MTH1 activator-1 can be used to probe the cellular and biological effects of upregulated oxidative damage repair in nucleotide pools and to delay or abrogate tumorigenesis [1].
Cat. No.: HY-134724
CAS No.: 2412986-35-5
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MTH1 ligand 1 is a target protein ligand for MTH1 and can be used to synthesize PROTAC
aTAG 2139 (HY-161162) [1].
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BAY-707, a chemical probe, is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy [1].
Cat. No.: HY-112817
CAS No.: 139307-94-1
Synonyms: 8-Oxo-Deoxyguanosine triphosphate
Category:
Target:
Cat. No.: HY-134725
CAS No.: 2412987-06-3
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MTH1 degrader-1, a MTH1 aTAG inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). MTH1 degrader-1 can be used for synthesis PROTAC aTAG 4531 (HY-163168) [1].
Cat. No.: HY-163168
CAS No.: 2412985-00-1
Synonyms: CFT-4531
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aTAG 4531 is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation [1].
Cat. No.: HY-135967
CAS No.: 901044-91-5
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MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity [1].
Cat. No.: HY-172265
CAS No.: 3115268-06-6
FKBP12 PROTAC FM4 is a PROTAC degrader of FKBP12, with a DC50 value of 0.09-0.22 nM. FKBP12 PROTAC FM4 inhibits global protein synthesis, induces apoptosis, and selectively reduces the viability of cervical cancer cells expressing MTH1-E6 and FKBP12 F36V-tagged SARS1. FKBP12 PROTAC FM4 is applicable to research related to HPV-positive cervical cancer [1].
Cat. No.: HY-125209A
CAS No.: 2253744-57-7
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TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 [1].TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis [1].TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells [1].TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells [1].TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay [1].TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) [1].TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer [1] .
Cat. No.: HY-161162
CAS No.: 2387510-81-6
Synonyms: CFT-2139
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aTAG 2139 (CFT-2139) is an aTAG-based MTH1 fusion protein degrader with a DC50 value of 1.1 nM. aTAG 2139 has a Ki value of 2.1 nM for MTH1 [1].
Cat. No.: HY-120936
CAS No.: 1884209-99-7
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IACS-4759 is a potent and selective MTH1 (MutT homolog 1) inhibitor with an IC50 of 0.6 nM. IACS-4759 has anti-cancer effects [1].
Cat. No.: HY-114939
CAS No.: 110871-16-4
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Phelorphan is a purine MTH1 inhibitor identified through chemical array screening. Although it targets cellular MTH1, its cytotoxicity to cancer cells is weaker than that of other reported inhibitors. The cytotoxicity of MTH1 inhibitors may be attributed to off-target effects, and MTH1 is not essential for cancer cell survival.
Cat. No.: HY-16965A
CAS No.: 1638211-05-8
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TH287 hydrochloride is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 hydrochloride is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 hydrochloride could act as a chemotherapeutic agent for cancer research [1].
Cat. No.: HY-112081A
CAS No.: 2223023-19-4
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BAY-707 acetate is a highly potent and selective substrate-competitive inhibitor of MTH1 with superior cellular target engagement and pharmacokinetic properties.
Cat. No.: HY-161161
CAS No.: 2758431-99-9
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aTAG 2139-NEG (Compound 23) binds to MTH1 and has no degradative activity with a Ki value of 2.0 nM. aTAG 2139-NEG serves as aTAG 2139 negative control [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
