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-134836

STM2457	Inhibitor	99.86%
STM2457 is a first-in-class, highly potent, selective and orally active METTL3 inhibitor with an IC₅₀ of 16.9 nM. STM2457 can be used for the research of acute myeloid leukaemia (AML).

HY-156677

STC-15	Inhibitor	99.90%
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases.

HY-115717

UZH2	Inhibitor	98.73%
UZH2 is a potent and selective METTL3 inhibitor with an IC₅₀ value of 5 nM.

HY-162080

METTL1-WDR4-IN-1	Inhibitor	98.87%
METTL1-WDR4-IN-1 (1) is a METTL1-WDR4 inhibitor, with an IC₅₀ of 144 μM.

HY-156773

STM3006	Inhibitor
STM3006 is a highly potent, selective, and orally active inhibitor of METTL3 (IC₅₀: 5 nM). STM3006 can reduce the m6A level, promote the formation of dsRNA, trigger a cell-intrinsic interferon response, and enhance the killing effect of T cells on tumors. STM3006 has anti-tumor activity, and its combination with anti-PD-1 immunotherapy yields better results.

HY-W037893

METTL3 activator-1	Activator	99.38%
METTL3 activator-1 (2-Piperazinecarboxylic acid methyl ester dihydrochloride) is a Mettl3 activator that can promote the expression of Mettl3. METTL3 activator-1 can be used for the study of liver fibrosis.

HY-P10387A

RSM3 TFA	Inhibitor	98.83%
RSM3 TFA, a stapled peptide, is a METTL3-METTL14 inhibitor with an K_d of 3.10 μM. RSM3 TFA inhibits tumor growth while induces cell apoptosis. RSM3 TFA can be used for study of cancer.

HY-168878

EP652	Inhibitor
EP652 (compound 56) potently inhibits the enzymatic activity of METTL3, with the IC₅₀s of 2 nM, ＜ 10 nM anf 37 nM in SPA, intracellular and ATPlite assay, respectively. EP652 plays an important role in liquid and solid tumors research.

HY-160415A

WD6305 TFA	Inhibitor	99.81%
WD6305 TFA is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 TFA has DC₅₀ values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 TFA inhibits m⁶A modification and proliferation of AML cells, and induces apoptosis. WD6305 TFA has antitumor activity.(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))

HY-153625

STM2120	Inhibitor	99.92%
STM2120 is a METTL3-METTL14 inhibitor with an IC₅₀ of 64.5 μM.

HY-158403

METTL3-IN-7	Inhibitor
METTL3-IN-7 (7460-0250) is a potent METTL3 inhibitor. METTL3-IN-7 strongly ameliorates Dextran sulfate sodium salt (DSS) (HY-116282C)-induced colitis. METTL3-IN-7 can be used Inflammatory bowel disease (IBD) research.

HY-P10387

RSM3	Inhibitor
RSM3, a stapled peptide, is a METTL3-METTL14 inhibitor with an K_d of 3.10 μM. RSM3 inhibits tumor growth while induces cell apoptosis. RSM3 can be used for study of cancer.

HY-134673B

UZH1b	Inhibitor	99.75%
UZH1b is an enantiomer of UZH1a (a METTL3 inhibitor). UZH1b is essentially inactive for METTL3 (IC₅₀=28 µM).

HY-159604

METTL3-IN-9	Inhibitor
METTL3-IN-9 (compound C3) is an inhibitor of methyltransferase-like METTL3, an RNA methyltransferase that catalyzes the N6-methyladenosine (m6A) modification of mRNA in eukaryotic cells.

HY-148467

METTL3-IN-1	Inhibitor
METTL3-IN-1 (compound 23) is a polyheterocyclic compound, acts as METTL3 inhibitor.

HY-148468

METTL3-IN-2	Inhibitor
METTL3-IN-2 (compound 28) is a METTL3 inhibitor with an IC₅₀ value of 6.1 nM. METTL3-IN-2 inhibits cell proliferation of Caov3 cancer cells.

HY-148469

METTL3-IN-3	Inhibitor
METTL3-IN-3 (compound 11) is a polyheterocyclic compound, acts as METTL3 inhibitor.

HY-158404

METTL3-IN-8	Inhibitor
METTL3-IN-8 (F039-0002) is a potent METTL3 inhibitor. METTL3-IN-8 strongly ameliorates Dextran sulfate sodium salt (DSS) (HY-116282C)-induced colitis. METTL3-IN-8 can be used Inflammatory bowel disease (IBD) research.

HY-156759

METTL3-IN-5	Inhibitor
METTL3-IN-5 (Compound 13) is a METTL3 inhibitor. METTL3-IN-5 inhibits MOLM-13 growth with an IC₅₀ less than 2 μM. METTL3-IN-5 has weak hERG inhibitory activity (IC₅₀ >30 μM). METTL3-IN-5 can be used for AML research.

HY-154997

7OQL	Inhibitor
7OQL (compound 54) is a selective METTL3 inhibitor (IC₅₀=0.054 µM). 7OQL has the potential to be used in the study of cancer.

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