METTL3

SAH is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 ?M.

STM2457 is a first-in-class, orally bioavailable small molecule inhibitor that selectively targets METTL3, a key component of the RNA N6-methyladenosine (m6A) methyltransferase complex. With an IC₅₀ of 16.9 nM, STM2457 exhibits high potency in inhibiting METTL3 activity. This compound has been demonstrated to impair leukemogenic gene expression programs and inhibit proliferation in METTL3-dependent acute myeloid leukemia (AML) models, making it a valuable chemical probe for epitranscriptomic regulation and a promising tool for AML research.

METTL3-IN-9 is an inhibitor of the methyltransferase-like protein METTL3, which functions as an RNA methyltransferase to catalyze the N6-methyladenosine (m6A) modification of mRNA in eukaryotic cells. This compound demonstrates significant biological activity in regulating gene expression through m6A modification. METTL3-IN-9 is essential for research applications focused on RNA biology, epitranscriptomics, and the study of mRNA modifications.

STM2120 is a selective inhibitor of the METTL3-METTL14 complex, exhibiting an IC50 of 64.5 μM. This compound disrupts the methyltransferase activity of METTL3, impacting RNA methylation processes. STM2120 is valuable for investigating the roles of RNA modifications in cellular functions and disease mechanisms, particularly in cancer research.

METTL3 activator-1 (2-Piperazinecarboxylic acid methyl ester dihydrochloride) is an activator of the Mettl3 enzyme, enhancing its expression. This compound plays a critical role in research applications focused on liver fibrosis, providing insights into the underlying molecular pathways and potential therapeutic targets.

UZH2 is a potent and selective inhibitor of the METTL3 enzyme, demonstrating an IC50 value of 5 nM. This compound is crucial for research focusing on mRNA methylation and epitranscriptomics, providing insights into gene regulation and potential therapeutic targets in various diseases. UZH2 is ideal for studies investigating the role of METTL3 in cellular processes and its implications in cancer biology.

STC-15 is a selective inhibitor of the RNA methyltransferase METTL3, known for its potential in modulating anti-tumor immunity and altering the tumor microenvironment. By inhibiting METTL3, STC-15 enhances anti-cancer immune responses through increased interferon signaling and shows synergy with T-cell checkpoint blockade. This compound is relevant for research in proliferative diseases, including various forms of cancer and autoimmune disorders.

STM3006 is a highly potent and selective inhibitor of METTL3, exhibiting an IC50 of 5 nM. This compound reduces m6A methylation levels, promotes double-stranded RNA formation, and triggers a cell-intrinsic interferon response, thereby enhancing T cell-mediated tumor cell elimination. STM3006 demonstrates significant anti-tumor activity and shows improved efficacy when combined with anti-PD-1 immunotherapy, making it a valuable tool for cancer research and therapeutic development.

EP652 is a potent METTL3 inhibitor, demonstrating an IC50 of 2 nM in the SPA assay, with additional IC50 values of less than 10 nM and 37 nM in intracellular and ATPlite assays, respectively. This compound is essential for research related to liquid and solid tumors, providing a valuable tool for investigating the role of METTL3 in cancer biology and therapeutic development.

UZH1b is an enantiomer of UZH1a, characterized by its minimal activity against the METTL3 methyltransferase, exhibiting an IC50 value of 28 µM. Although it serves as a structural analog of UZH1a, UZH1b does not effectively inhibit METTL3 and may be utilized in research to explore the comparative effects of enantiomers on biological pathways. Its unique properties allow for further investigation in studies related to RNA methylation and gene regulation.

METTL3-IN-8 is a potent inhibitor of the methyltransferase METTL3. This compound significantly alleviates colitis induced by Dextran sulfate sodium salt (DSS), highlighting its potential application in the study of inflammatory bowel disease (IBD). METTL3-IN-8 serves as a valuable tool for research aimed at understanding the mechanistic role of METTL3 in IBD and related inflammatory conditions.

UZH1a is a selective inhibitor of METTL3, demonstrating an IC50 of 280 nM. This compound has shown potential for epitranscriptomic modulation, influencing various cellular processes. Additionally, UZH1a exhibits antitumor activity and serves as a valuable chemical probe for investigating the biological functions of METTL3 in research applications.

UZH1 is a METTL3 inhibitor that comprises a racemic mixture of UZH1a and UZH1b. UZH1a is a highly selective inhibitor, displaying an IC50 of 280 nM, while UZH1b shows minimal activity with an IC50 of 28 µM. UZH1 serves as an effective tool for epitranscriptomic modulation of cellular processes and demonstrates antitumor activity. Additionally, UZH1 can be utilized as a chemical probe for in-depth investigations of METTL3's role in various biological contexts.

ZINC13000658 is an inhibitor of METTL, a family of methyltransferases. This compound demonstrates substantial antiproliferative effects across various cell lines, effectively inducing G1 phase cell cycle arrest and apoptosis in HepG2 (IC50 = 5.632 µM) and SNU-449 (IC50 = 6.184 µM) cells. ZINC13000658's mechanism may involve the inhibition of multiple methyltransferases, including METTL1, METTL3, METTL6, METTL16, and METTL18. This reagent is valuable for investigating various cancer research applications.

METTL3 activator-1 free base is a potent activator of the METTL3, METTL14, and WTAP complexes. This compound enhances HIV-1 p24 virion production and significantly increases the N6-adenosine methylation levels within the viral RNA genome. It serves as a valuable tool for research in viral biology and RNA modification studies.

Antiviral Agent 24 is a potent antiviral compound that primarily targets viral replication pathways. Exhibiting EC50 values of 0.101 µM for Enterovirus 71 (EV71), 19.9 µM for Coxsackievirus A21 (CVA21), and 91.2 µM for Enterovirus 68 (EV68), this reagent demonstrates significant antiviral activity. Additionally, Antiviral Agent 24 inhibits the enzymatic activity of METTL3/METTL14 in a dose-dependent manner, showcasing its potential utility in antiviral research applications.

Antiviral agent 23 is a potent inhibitor of enterovirus 71 (EV71) with an EC50 value of 94 nM. It effectively suppresses the activity of the methyltransferase complex METTL3/METTL14, demonstrating significant antiviral activity. This compound is suitable for research focused on enteroviral infections and the mechanisms of RNA modification in viral pathogenesis.

METTL1-WDR4-IN-2 is a selective inhibitor of the METTL1-WDR4 methyltransferase complex, exhibiting an IC50 value of 41 μM. This compound demonstrates significant selectivity, with IC50 values of 958 μM against METTL3-14 and 208 μM against METTL16. METTL1-WDR4-IN-2 is valuable for investigating the role of RNA methylation in cancer and other biological processes related to epitranscriptomics.

WD6305 is a selective PROTAC degrader targeting METTL3 and METTL14, with DC50 values of 140 nM and 194 nM, respectively. This compound effectively inhibits m6A modification and has been shown to suppress proliferation and induce apoptosis in acute myeloid leukemia (AML) cells. WD6305 demonstrates significant antitumor activity, making it a valuable tool for research on RNA modifications and cancer therapeutics.

METTL3-IN-1 is a potent METTL3 inhibitor designed to selectively inhibit the activity of the METTL3 methyltransferase. This compound demonstrates significant biological activity in modulating RNA methylation, making it a valuable tool for studying the role of METTL3 in various cellular processes. It is applicable in research areas such as epitranscriptomics and cancer biology, where understanding RNA modifications is crucial.

METTL3-IN-2 is a selective inhibitor of the methyltransferase METTL3, exhibiting an IC50 value of 6.1 nM. This compound effectively inhibits cell proliferation in Caov3 ovarian cancer cells, providing a valuable tool for research into the regulation of RNA methylation and its implications in cancer biology. METTL3-IN-2 can be utilized in studies focused on understanding METTL3's role in tumor growth and the development of targeted cancer therapies.

METTL3-IN-3 is a selective inhibitor of the methyltransferase METTL3, which plays a critical role in RNA m6A methylation. This compound demonstrates significant inhibition of METTL3 activity, thereby impacting the regulation of gene expression and RNA metabolism. METTL3-IN-3 is valuable for research applications focusing on epitranscriptomics, RNA modifications, and their implications in various biological processes and diseases.

METTL3-IN-5 is a selective inhibitor of METTL3, a key enzyme involved in N6-methyladenosine (m6A) methylation. This compound demonstrates potent inhibitory effects on the growth of MOLM-13 cells, with an IC50 of less than 2 μM. While exhibiting minimal hERG inhibitory activity (IC50 >30 μM), METTL3-IN-5 is a valuable tool for researching acute myeloid leukemia (AML) and m6A-related biological processes.

METTL3-IN-13 is a selective inhibitor of the methyltransferase METTL3. This compound exhibits significant biological activity by disrupting RNA methylation, which plays a critical role in various cancer types including hypopharyngeal squamous cell carcinoma and non-small cell lung cancer. It serves as a valuable tool for investigating the role of METTL3 in oncogenic processes and may assist in the development of targeted therapies.

SAH-13C10 is a stable isotope labeled derivative of S-Adenosylhomocysteine (SAH). As an important amino acid derivative, SAH plays a crucial role as a modulator in various metabolic pathways and serves as an intermediate in the synthesis of cysteine and adenosine. It functions as an inhibitor of the METTL3-METTL14 heterodimer complex, demonstrating an IC50 of 0.9 μM, making it valuable for research in epitranscriptomics and cellular metabolism studies.

6-Hydroxy-1-(4-(2-hydroxyethyl)piperazin-1-yl)hexan-1-one serves as a key linker in the development of PROTAC molecules targeting METTL3. This compound is integral for facilitating the degradation of specific proteins, thereby enabling cellular pathway modulation and functional studies. Researchers can employ this linker to explore targeted protein degradation applications in various biological contexts.