TH588 | MTH1/NUDT1 inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 5 mg | $65.00 | ||
| 25 mg | $200.00 |
TH588 (1609960-31-7) is a first-in-class nudix hydrolase family inhibitor.1 MTH1/NUDT1 is a family member that “sanitizes” oxidized deoxynucleotide triphosphates (dNTP) preventing their incorporation into DNA and thus avoiding DNA damage and cell death. TH588 inhibits MTH1/NUDT1 (IC50 = 5 nM) leading to cell death in several cancer cell lines while not affecting normal cells. Active in vitro and in vivo. Recent evidence has raised doubts about the cancer-killing ability of MTH1 inhibition.2,3 Conversely, TH588 has been also shown to decrease osteosarcoma cell viability, impair cell cycle, and increase apoptosis via an MTH1-dependent pathway.4
References/Citations:
1) Gad et al. (2014), MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool; Nature, 508 215
2) Petrocchi et al. (2016) Identification of potent and selective MTH1 inhibitors; Bioorg. Med. Chem. Lett., 26 1503
3) Kettle et al. (2016), Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival; J. Med. Chem., 59 2346
4) Moukengue et al. (2020), TH1579, MTH1 inhibitor, delays tumour growth and inhibits metastases development in osteosarcoma model; EBioMedicine, 53 102704
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
TH588 (1609960-31-7) is a first-in-class nudix hydrolase family inhibitor.1 MTH1/NUDT1 is a family member that “sanitizes” oxidized deoxynucleotide triphosphates (dNTP) preventing their incorporation into DNA and thus avoiding DNA damage and cell death. TH588 inhibits MTH1/NUDT1 (IC50 = 5 nM) leading to cell death in several cancer cell lines while not affecting normal cells. Active in vitro and in vivo. Recent evidence has raised doubts about the cancer-killing ability of MTH1 inhibition.2,3 Conversely, TH588 has been also shown to decrease osteosarcoma cell viability, impair cell cycle, and increase apoptosis via an MTH1-dependent pathway.4
References/Citations:
1) Gad et al. (2014), MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool; Nature, 508 215
2) Petrocchi et al. (2016) Identification of potent and selective MTH1 inhibitors; Bioorg. Med. Chem. Lett., 26 1503
3) Kettle et al. (2016), Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival; J. Med. Chem., 59 2346
4) Moukengue et al. (2020), TH1579, MTH1 inhibitor, delays tumour growth and inhibits metastases development in osteosarcoma model; EBioMedicine, 53 102704
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Focus Biomolecules • Plymouth Meeting, PA USA • 1-855-FOCUS21
Focus Biomolecules
Plymouth Meeting, PA USA
1-855-FOCUS21
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