GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

MS023 dihydrochloride (MS023 2HCl) is a selective, cytosolic and highly potent inhibitor of human type I protein arginine methyltransferases (PRMTs) with antitumour activity, inhibits PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and increases the proliferative capacity of isolated cultured MuSC. It can be used to study breast cancer.

AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).

AMI-1 free acid is a cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs) with potential anticancer activity, inhibits PRMT1 and yeast Hmt1p, inhibits arginine methylation, and modulates nuclear receptor-regulated transcription from estrogen- and androgen-responsive elements.

SGC6870 is a novel potent, selective, and cell-active inhibitor of PRMT6 with IC50 of 77 ± 6 nM, being selective over all other PRMTs and 23 methyltransferases.

MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 μM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against typ

MS-049 oxalate salt is a potent and selective inhibitor of protein arginine methyltransferases (PRMTs) PRMT 4 and PRMT6.

Potent and selective PRMT5 inhibitor (IC50 = 4 nM). Selective for PRMT5 over a panel of other PRMTs and lysine methyltransferases. Inhibits proliferation of mantle cell lymphoma (MCL) in vitro. To request the negative control for GSK 591, please fill out the SGC 2096 request form on the SGC website.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs) with anticancer and antitumor activity, inhibiting PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, and can be used to study advanced solid tumors.

SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription a

GSK3368715, a first-in-class, orally active, potent, and selective SAM-noncompetitive inhibitor of Type I Protein Arginine Methyltransferases (PRMTs), exhibits anti-tumor efficacy across multiple cancer models and alters exon usage with IC50 values in the lower nM range. It synergizes with GSK3326595 (Type II inhibitor) (Axon 3750) to inhibit tumor growth.

PRMT5-IN-19 (Compound 41) is a potent orally active PRMT5 inhibitor, exhibiting selectivity towards the SAM-binding pocket of PRMT5 with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). It effectively blocks methyltransferase activity and demonstrates high specificity against other PRMTs and PKMTs. PRMT5-IN-19 exerts anti-proliferative effects through the induction of apoptosis and holds potential in cancer-related research [1].

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.