METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 µM). METTL1-WDR4-IN-1 inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking m7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8+ T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy[1][2].
Molekulargewicht:
241.27
Reinheit:
99.61
CAS Nummer:
[374705-10-9]
Formel:
C8H11N5O2S
Target-Kategorie:
DNA Methyltransferase,Pyruvate Kinase
Anwendungsbeschreibung:
MCE Product type: Reference compound
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
