m6a

N6-Methyladenosine is a methylated adenine residue, glycoside is an endogenous uridine product of transfer RNA degradation. It is the most prevalent internal modification of messenger RNA present in all higher eukaryotes and can modify viral RNA with antiviral activity.

FB23-2 is a potent and selective inhibitor of the mRNA N6-methyladenosine (m6A) demethylase FTO with an IC50 of 2.6 μM.

(2'OMe-5'p-m6A)pG is a monomeric material used in the synthesis of nucleic acids.

(2'OMe-5'pp-m6A)pG serves as a monomeric material for nucleic acid synthesis.

m7Gpppm6AmpG, a trinucleotide mRNA 5' cap analog, facilitates RNA synthesis in vitro [1].

M7Gpppm6AmpG ammonium, a trinucleotide mRNA 5' cap analog, facilitates in vitro RNA synthesis [1].

GSK-J2 is an inactive enantiomer of GSK-J1 that is lipophilic and serves as an inactive control for GSK-J21.

KDM2/7-IN-1 (TC-E 5002) is a selective small-molecule inhibitor of the KDM2/7 histone demethylase subfamily, exhibiting IC50 values of 0.2, 1.2, 6.8, 55, 83, >100, and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A, and KDM4A, respectively. KDM2/7-IN-1 inhibits the proliferation of HeLa and KYSE-150 cancer cells in vitro, highlighting its utility in epigenetic and oncology research.

GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.

TMBIM6 antagonist-1 (BAX-inhibitor-1) is a bax inhibitor

METTL3-IN-9 (compound C3) serves as an inhibitor of the RNA methyltransferase known as methyltransferase-like METTL3. This enzyme is responsible for catalyzing the N6-methyladenosine (m6A) modification of mRNA within eukaryotic cells.

ALKBH5-IN-3 (Compound 20m) is a selective ALKBH5 inhibitor (IC50=21 nM) that effectively stabilizes ALKBH5 in HepG2 cells and elevates m6A levels in intact cells.

ALKBH5 inhibitor 1 (compound 3) is an inhibitor of the RNA M6A demethylase AlkBH5, exhibiting an IC50 value of 0.84 μm. Additionally, it demonstrates effective anti-proliferative activity.

Perfluoroenanthic acid (Perfluoroheptanoic acid) is a perfluoroalkyl substance (PFAS) that negatively impacts spermatogenic development and testicular m6A RNA methylation in offspring exposed during gestation, thus impeding spermatogenesis and inducing reproductive toxicity. Additionally, in primary cortical neuron cultures, Perfluoroenanthic acid alters dendritic spine morphology and synaptogenesis, enhances neural activity and synaptic transmission, and increases the expression of excitatory synapse-associated proteins Synaptophysin and PSD95.

YTH-IN-1 is an inhibitor of the five YTH structural domains in the human YTHDF1, YTHDF2, YTHDF3, YTHDC1, and YTHDC2 proteins.The YTH family of proteins is an N 6-methyladenosine (m6A) reader that plays an important regulatory role in gene expression.

ALKBH5-IN-5 is a highly selective, potent and covalently binding ALKBH5 inhibitor (IC50 = 0.62 μM) that alters m6A levels on mRNA, promotes differentiation and induces apoptosis, with antitumor activity.ALKBH5 is an N6-methyladenosine (m6A) demethylase that is closely related to leukemogenesis.

DDO-02267 is a selective lysine-targeted covalent inhibitor of ALKBH5, with an IC50 value of 0.49 μM. It increases levels of N6-methyladenosine (m6A) and targets the ALKBH5-AXL signaling axis. DDO-02267 serves as a probe for studying the biological function of mRNA demethylases.

DDO-2728 is a selective pyrazolo[1,5-a]pyrimidine-based ALKBH5 inhibitor with an IC50 of 2.97 μM. It increases the levels of N6-methyladenosine (m6A) modifications in acute myeloid leukemia (AML) cells and exhibits antiproliferative activity in these cells. DDO-2728 also demonstrates anti-tumor efficacy in the MV4-11 xenograft model.

W23-1006 is a novel, selective, and cell-active covalent inhibitor of ALKBH5 (an m6A RNA demethylase). It functions by binding to the C200 residue of ALKBH5 with an IC50 value of 3.848 μM. W23-1006 demonstrates superior selectivity, being approximately 30-fold and 8-fold more potent against ALKBH5 than against FTO and ALKBH3, respectively. By inhibiting ALKBH5 and increasing global m6A abundance, W23-1006 effectively suppresses proliferation, migration, and colonization in triple-negative breast cancer (TNBC) cells.

YTHDF2-IN-1 (Compound CK-75) is an inhibitor of YT521-B homology domain family 2 (YTHDF2) with a dissociation constant (Kd) of 26.2 μM, and it effectively blocks the interaction between YTHDF2 and m6A RNA. It suppresses colony formation in JAR cells and exhibits antiproliferative activity in various cancer cell lines, with an IC50 in the micromolar range. Additionally, YTHDF2-IN-1 induces apoptosis in K562 cells and causes cell cycle arrest at the G0/G1 phase.

Ena15 is an ALKBH5 inhibitor that enhances the demethylase activity of FTO. It can increase m6A RNA levels and stabilize FOXM1 mRNA. Additionally, Ena15 inhibits the growth activity of glioblastoma multiforme.

WD6305 is an effective and selective METTL3-METTL14 PROTAC degrader, with DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. It inhibits m6A modification and the proliferation of acute myeloid leukemia cells while inducing apoptosis. WD6305 also exhibits antitumor activity.

AF151 is a METTL3 PROTAC degrader with a DC50 of 0.43 μM in MOLM-13 cells. It inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 induces apoptosis and decreases Bcl-2 protein levels. This compound is applicable in research related to cancers such as acute myeloid leukemia (AML).

I3IN-002 is a small molecule inhibitor targeting the RNA-binding protein IGF2BP3, with an IC50 value of approximately 2 μM in SEM cells. It disrupts the interaction with m6A-modified mRNA, destabilizing target genes (such as CDK6, MYC, and BCL2), thereby inhibiting the growth of leukemia cells, inducing cell cycle arrest, and promoting apoptosis. I3IN-002 shows potential for research in B-cell acute lymphoblastic leukemia.