TH287

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H318：Verursacht schwere Augenschäden.

• Sicherheit

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

TH287 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC₅₀ = 0.8 nM) that selectively kills cancer cell lines (IC₅₀s = 0.8-3.06 μM) without significant cytotoxicity towards primary or immortalized cells (IC₅₀s = ≥20 μM). At up to 100 μM it does not show significant effect towards the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).

• Verwenden

  6-(2,3-Dichlorophenyl)-N4-methyl-2,4-pyrimidinediamine is known to possess antitumor effects and nanomolar MTH1-inhibitory activity in vitro for cancer cell survival.

• Einzelnachweise

  1. gad h, koolmeister t, jemth as et al. mth1 inhibition eradicates cancer by preventing sanitation of the dntp pool. nature. 2014 apr 10;508(7495):215-21.

TH287 Upstream-Materialien And Downstream Produkte

TH287 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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