METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 µM). METTL1-WDR4-IN-1 TFA inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking the 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 TFA 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 TFA 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].
Molecular Weight:
355.29
Purity:
99.61
Formula:
C10H12F3N5O4S
Target:
DNA Methyltransferase,Pyruvate Kinase
Application Notes:
MCE Product type: Reference compound
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