374705-10-9
Chemical Structure
METTL1-WDR4-IN-1
- CAS No.: 374705-10-9
- Formula:C8H11N5O2S
- Molecular Weight:241.27
InChIKey: VRQOBSWPEIRZJY-UHFFFAOYSA-N
SMILES: S=C1N=C2C(N1)=C(N)N=CN2CC(CO)O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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METTL1-WDR4-IN-1 | 99.61% | 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. | ||||||||||||||||||||
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References
- [1]. Nai F, et al. Small-Molecule Inhibitors of the m7G-RNA Writer METTL1. ACS Bio Med Chem Au. 2023 Dec 12;4(2):100-110. [Content Brief]
- [2]. Wang F, et al. METTL1 mediates PKM m7G modification to regulate CD155 expression and promote immune evasion in colorectal cancer. J Transl Med. 2024 Dec 31;22(1):1161. [Content Brief]
