METTL3 Inhibitor

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).

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.

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.

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

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.

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.

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.

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

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.

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.

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.

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.

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

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.

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

METTL3-IN-12 (Compound 15) is a selective METTL3 inhibitor with an IC₅₀ of 50 nM. METTL3-IN-12 exhibits significant anti-proliferative activity in various leukemia cell lines. METTL3-IN-12 can be used for research on leukemia.

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

METTL3-IN-11 is an excellent, selective METTL3 inhibitor (IC₅₀ = 45.31 nM). METTL3-IN-11 exhibits high selectivity towards METTL3 compared to DNMT1, EZH1, MLL1, and PRMT1. METTL3-IN-11 reduces the m6A level of total RNA in MOLM-13 and SKOV3 cells, induces cell apoptosis, and inhibits cell migration. METTL3-IN-11 can reduce the expression of m6A downstream target genes (c-MYC and BCL2). METTL3-IN-11 can be used for the study of ovarian cancer and acute myeloid leukemia.