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Results for "

human MTH1

" in MedChemExpress (MCE) Product Catalog:

6

Inhibitors & Agonists

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100549
    (S)-Crizotinib
    3 Publications Verification

    		 DNA/RNA Synthesis Apoptosis Cancer
    (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 .
    (S)-Crizotinib
  • HY-125209A
    TH5427 hydrochloride

    		Apoptosis PARP DNA/RNA Synthesis Cancer
    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 .
    TH5427 hydrochloride
  • HY-123599
    IACS-4619

    		DNA/RNA Synthesis Cancer
    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 .
    IACS-4619
  • HY-12814A
    TH588 hydrochloride

    		DNA/RNA Synthesis Microtubule/Tubulin Cancer
    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 .
    TH588 hydrochloride
  • HY-100549R
    (S)-Crizotinib (Standard)

    		DNA/RNA Synthesis Reference Standards Apoptosis Cancer
    (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 .
    (S)-Crizotinib (Standard)
  • HY-180404
    SU0383

    		DNA/RNA Synthesis Cancer
    SU0383 is a dual MTH1 and OGG1 inhibitor with IC50 values of 0.034 μM and 0.49 μM, respectively. SU0383 induces cytotoxicity in cancer cells and increases sensitivity of tumor cells to oxidative stress, and showing low toxicity in normal cells. SU0383 can be used for cancer research .
    SU0383

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