prmts

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.

AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1].

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

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

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.

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.

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

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

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.

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, exerting anti-proliferative effects through apoptosis induction and holding potential in cancer-related research [1].

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.

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

NG,NG-dimethyl-L-arginine-d6 (ADMA-d6) (hydrochloride) is intended for use as an internal standard for the quantification of NG,NG-dimethyl-L-arginine by GC- or LC-MS. ADMA is an endogenous inhibitor of nitric oxide synthase (NOS). It is formed from arginine by protein arginine methyltransferases (PRMTs) and degraded by dimethylarginine dimethylaminohydrolases (DDAHs) and alanine-glyoxylate aminotransferase 2 (AGXT2). ADMA levels are increased concomitant with an increase in blood pressure in Dahl salt-sensitive rats fed a high-salt diet. ADMA levels are increased in the plasma in a variety of endothelial dysfunction-related diseases, including hypertension, congestive heart failure, and end-stage renal disease.

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.