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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
8 Results for "
human MTH1
" in MedChemExpress (MCE) Product Catalog:
Products (8)
8 Results for "human 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
1 Cited Publications
Cat. No.: HY-N6845
CAS No.: 19275-46-8
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 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .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 .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .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 .
Cat. No.: HY-12814A
CAS No.: 1640282-30-9
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TH588 hydrochloride is a highly selective human MTH1 inhibitor (IC50=5 nM) with additional microtubule-targeting properties. TH588 hydrochloride interferes with mitotic progression, induces genomic 8-oxodG formation, DNA damage and cell cycle arrest, and exhibits significant cytotoxicity. Combined with phenethyl isothiocyanate, TH588 hydrochloride enhances ROS-mediated effects and effectively inhibits the growth of visceral metastases of malignant melanoma in mice. TH588 hydrochloride is widely applicable to research related to cancers, pancreatic cancer, leukemia, lymphoma, malignant melanoma and lung cancer .
Cat. No.: HY-123599
CAS No.: 1884209-98-6
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IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target .
Cat. No.: HY-100549R
CAS No.: 1374356-45-2
Research Areas:
(S)-Crizotinib (Standard) is the analytical standard of (S)-Crizotinib (HY-100549). This product is intended for research and analytical applications. (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 .
Cat. No.: HY-189451
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Research Areas:
apPHOTAC-I-2C is an arylazopyrazole-based photoswitchable PROTAC and CRBN-binding degrader that binds CRBN with human IC50 values of 15.9 nM and 33.5 nM, and achieves light-controlled targeted degradation of BET proteins (BRD2, BRD3, BRD4) and MTH1 in a manner dependent on CRBN and the proteasome pathway. apPHOTAC-I-2C can be used for research on acute lymphoblastic leukemia .
Cat. No.: HY-P74740
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: NUDT1; Methylated Purine Nucleoside Triphosphate Hydrolase; Prev. MTH1; 8-Oxo-7,8-Dihydrodeoxyguanosine Triphosphatase; 7,8-Dihydro-8-Oxoguanine Triphosphatase; Nucleoside Diphosphate-Linked Moiety X Motif 1; Nudix Motif 1; 8-Oxo-7,8-Dihydroguanosine Triphosphatase; 8-Oxo-DGTPase; 2-Hydroxy-DATP Diphosphatase; Nudix (Nucleoside Diphosphate Linked Moiety X)-Type Motif 1; MutT human Homolog 1; Nucleoside Diphosphate-Linked Moiety X-Type Motif 1; Nudix Hydrolase 1; Oxidized Purine Nucleoside Triphosphate Hydrolase
Species:
Human
Source:
E. coli
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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
