dimethylation

TP-064 is a potent and selective PRMT4 inhibitor, featuring an IC50 < 10nM for methylation of H3 (1-25) and over 100-fold selectivity compared to other histone methyltransferases and non-epigenetic targets. It inhibits the methylation of MED12 in cells with an IC50 of 43 nM.

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.

Dot1L-IN-9 (Compound 12) is a DOT1L inhibitor with an IC50 of 125 nM. It effectively reduces H3K79 dimethylation and is utilized in leukemia research.

KTX-1001, also referred to as NSD2 inhibitor 161, is an innovative and potent inhibitor of nuclear SET domain-containing protein 2 (NSD2). This compound specifically binds to NSD2, inhibiting its catalytic activity and the mono- and dimethylation of histone H3 lysine 36 (H3K36). Such regulation impacts gene expression involved in cellular processes, including proliferation, which may subsequently slow cancer cell growth. NSD2 is part of the NSD family of histone lysine methyltransferases, which are often overexpressed and dysregulated in various cancer types.

C-MS023 is a photoactivatable prodrug of MS023, designed to achieve spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. It specifically inhibits PRMT6-mediated asymmetric dimethylation of H3 Arginine 2 (H3R2me2a) with an IC50 of approximately 0.2224 μM. The photolysis of C-MS023 can be triggered by exposure to 420 nm visible light, releasing MS023, which effectively downregulates histone arginine asymmetric dimethylation and transcriptional activities related to DNA replication.

Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM). Exhibits selectivity over all other PRMTs and 23 methyltransferases. In HEK293T cells overexpressing PRMT6, inhibits asymmetric dimethylation of H3R2 (IC50 = 0.8 μM) Negative control SGC 6870N (Cat. No. 7184) also available.

Parconazole Free Base is used in veterinary as an oral fungicide with a broad-spectrum activity against dermatophytes, yeasts, and others fungi. This compound does not have any antibacterial effect. The mechanism of action involves inhibition of the fungal cytochrome P450 dependent 14alpha-dimethylation of lanosterol to ergosterol.

Dot1L-IN-1 TFA is a potent and selective Dot1L inhibitor, with a K i of 2 pM and an IC50 of <0.1 nM. It effectively inhibits H3K79 dimethylation (IC50 = 3 nM) and suppresses HoxA9 promoter activity (IC50 = 17 nM) in HeLa and Molm-13 cells, respectively [1].

DC432 is a cell-permeable peptide that serves as an inhibitor of N-terminal Xaa-Pro-Lys N-methyltransferase 1 (NTMT1; IC50 = 0.054 µM), capable of binding to both NTMT1 and NTMT2 with dissociation constants (Kds) of 0.3 and 1 µM, respectively. It effectively inhibits the N-terminal dimethylation of regulator of chromosome condensation 1 (RCC1) by NTMT1 at concentrations of 10 and 50 µM in cell-free assays. Furthermore, at a concentration of 100 µM, DC432 diminishes the trimethylation of the RCC1 SPKRIA motif in HCT116 cells.

NSD-IN-3 (compound 3) serves as a potent inhibitor of the nuclear receptor binding SET domain (NSD). It effectively targets NSD2-SET and NSD3-SET, displaying IC 50 values of 0.81 μM and 0.84 μM, respectively. This compound also impedes the dimethylation of histone H3K36 and suppresses the expression of genes targeted by NSDs in non-small cell lung cancer cells. Furthermore, NSD-IN-3 promotes s-phase cell cycle arrest and induces apoptosis [1].