METTL3

Methyltransferase-like 3

Methyltransferase-like 3 (METTL3) is an enzyme that functions as a key methyltransferase in the process of N6-methyladenosine (m6A) RNA methylation. METTL3 contains a catalytic domain that is responsible for the transfer of methyl groups to adenosine residues in RNA. METTL3 usually forms a complex with METTL14 and other proteins to enhance its catalytic activity and substrate specificity. The m6A modification mediated by METTL3 plays crucial roles in various biological processes, including RNA splicing, stability, translation efficiency and degradation. METTL3 is involved in the regulation of gene expression and has a significant impact on cell differentiation, development and disease occurrence. Dysregulation of METTL3 has been implicated in many human diseases, especially in the occurrence and development of various cancers^[1]^[2].

References:

[1]. Wang CX, et al. METTL3-mediated m6A modification is required for cerebellar development. PLoS Biol. 2018 Jun 7;16(6):e2004880. [Content Brief]

[2]. Xu P, et al. Roles and drug development of METTL3 (methyltransferase-like 3) in anti-tumor therapy. Eur J Med Chem. 2022 Feb 15;230:114118. [Content Brief]

METTL3 Related Products (23):

By Effects:	Inhibitors (20) Degrader (1) Activators (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-W125425

Methyl piperazine-2-carboxylate	Activator
Methyl piperazine-2-carboxylate (compound 4) is a potent METTL3/METTL14/WTAP activator. Methyl piperazine-2-carboxylate increases HIV-1 p24 virion production. Methyl piperazine-2-carboxylate increases the N6-adenosine methylation level in the viral RNA genome.

HY-160415

WD6305	Inhibitor
WD6305 is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 has DC₅₀ values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 inhibits m⁶A modification and proliferation of AML cells, and induces apoptosis. WD6305 has antitumor activity.(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))

HY-162930

PROTAC METTL3 degrader 1	Degrader
PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based PROTAC METTL3 degrader (DC₅₀: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC₅₀ value of 341 nM. PROTAC METTL3 degrader 1 has anti-proliferative activities against AML cells. Black: Linker (HY-ER002); Red: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217).

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