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 (30):

By Effects:	Inhibitors (24) Degraders (2) Activators (2) Chemical (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-134836

STM2457	Inhibitor	99.57%
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-156773

STM3006	Inhibitor	98.71%
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-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-115717

UZH2	Inhibitor	98.91%
UZH2 is a potent and selective METTL3 inhibitor with an IC₅₀ value of 5 nM.

HY-183186

EP102	Inhibitor
EP102 is an orally active, selective inhibitor of the METTL3/METTL14 complex with an IC₅₀ of 2 nM. EP102 reduces intracellular N6-methyladenosine levels, inhibits cancer cell proliferation, and thereby suppresses tumor growth in mouse models. EP102 is applicable for the research of acute myeloid leukemia, ovarian solid tumors and advanced solid tumors.

HY-W037893

CHMA1004 dihydrochloride	Activator	99.38%
CHMA1004 (Methyl piperazine-2-carboxylate; METTL3 activator-1) dihydrochloride is a METTL3/METTL14/WTAP methyltransferase complex activator. CHMA1004 dihydrochloride exhibits neuroprotective and anxiolytic potential by enhancing m⁶A methylation modification of RNA. CHMA1004 dihydrochloride promotes HIV replication in an infection context. CHMA1004 dihydrochloride can be used in studies related to anxiety disorders and HIV-1 infection.

HY-160415

WD6305	Inhibitor	98.98%
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-P10387

RSM3	Inhibitor
RSM3 is a METTL3-METTL14 complex inhibitor with a K_d of 3.10 μM for the METTL3-METTL14 complex. RSM3 reduces the m⁶A modification level of SLC31A1 and the global RNA methylation level. RSM3 upregulates programmed cell death-related genes, enhances cell apoptosis, inhibits pro-cancer signals and suppresses tumor growth. RSM3 is applicable to the research of preeclampsia and cancer.

HY-158404

METTL3-IN-8	Inhibitor	99.81%
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-153625

STM2120	Inhibitor	99.19%
STM2120 is a METTL3-METTL14 inhibitor with an IC₅₀ of 64.5 μM.

HY-P10387A

RSM3 TFA	Inhibitor	98.83%
RSM3 TFA is a METTL3-METTL14 complex inhibitor with a K_d of 3.10 μM for the METTL3-METTL14 complex. RSM3 TFA reduces the m⁶A modification level of SLC31A1 and the global RNA methylation level. RSM3 TFA upregulates programmed cell death-related genes, enhances cell apoptosis, inhibits pro-cancer signals and suppresses tumor growth. RSM3 TFA is applicable to the research of preeclampsia and cancer.

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-168878

EP652	Inhibitor
EP652 is a METTL3 inhibitor and antitumor agent with IC₅₀ values of 2 nM, <10 nM, and 37 nM in SPA, intracellular, and ATPlite assays, respectively. EP652 exhibits high selectivity against 40 other methyltransferases and FTO, and possesses favorable pharmacokinetic parameters. EP652 reduces intracellular N⁶-methyladenosine (m⁶A) levels in mRNA. EP652 inhibits tumor growth and progression of both hematologic malignancies and solid tumors. EP652 can be used for the research of acute myeloid leukemia, ovarian cancer, non-small cell lung cancer, and hypopharyngeal squamous cell carcinoma.

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-134673B

UZH1b	Inhibitor	99.85%
UZH1b is an enantiomer of UZH1a (a METTL3 inhibitor). UZH1b is essentially inactive for METTL3 (IC₅₀=28 µM).

HY-178947

ZINC13000658	Inhibitor
ZINC13000658 is a METTL inhibitor. ZINC13000658 exhibits significant anti proliferative activity in various cells and can induce G1 phase cell cycle arrest and apoptosis such as HepG2 (IC₅₀ = 5.632 µM) and SNU-449 (IC₅₀ = 6.184 µM) cells. ZINC13000658 may be related to the inhibition of the activity of multiple methyltransferases such as METTL1, 3, 6, 16, 18, etc. ZINC13000658 can be used for research on various types of cancer.

HY-174873

AF151	Degrader	98.87%
AF151 is a METTL3 PROTAC degrader with the DC₅₀ of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)).

HY-162930

PROTAC METTL3 degrader 1	Degrader
PROTAC METTL3 degrader 1 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 can be used for the research of acute myeloid leukemia and gastric cancer.

HY-148467

METTL3-IN-1	Inhibitor	98.07%
METTL3-IN-1 (compound 23) is a polyheterocyclic compound, acts as METTL3 inhibitor.

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