54 products were found matching "K11437"!

Protein function: Arginine methyltransferase that can catalyze the formation of both omega-N monomethylarginine (MMA) and asymmetrical dimethylarginine (aDMA), with a strong preference for the formation of aDMA (PubMed:17898714, PubMed:18077460, PubMed:18079182, PubMed:19405910, PubMed:30420520). Preferentially...

Description: EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM). Target: Histone Methyltransferase. Smiles: CNCCN(C)Cc1c[nH]nc1-c1ccc(O[C@H]2C[C@@H](C2)OCCC2CCOCC2)cc1. References: Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First...

Description: MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 values of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively. Target: Histone Methyltransferase. Smiles: CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN. References: Eram MS, et al. ACS Chem Biol....

Description: 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. Target: Others. Smiles: C(=O)(N1[C@@H](C=2C(NC(=O)C1)=CC=C(C)C2)C3=CC(C)=CC(C)=C3)C=4SC(Br)=CC4

Description: 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...

Description: Protein arginine N-methyltransferase 6, also known as Histone-arginine N-methyltransferase PRMT6, PRMT6, and HRMT1L6, is a member of the protein arginine N-methyltransferase family and PRMT6 subfamily. PRMT6 is highly expressed in kidney and testes. PRMT6 is known to catalyze the generation of...

Human PRMT6 (GenBank Accession No. NM_018137), amino-acids 2-375(end), with N-terminal His-tag, MW=43 kDa, expressed in E. coli. Assay conditions: 50 µl reaction mix (20 mM phosphate buffer pH 7.4, 20 µM S-adenosylmethionine, and 1-5 ng methyl-transferase PRMT6) is added to microwells coated with histone substrate....

Protein function: Arginine methyltransferase that can catalyze the formation of both omega-N monomethylarginine (MMA) and asymmetrical dimethylarginine (aDMA), with a strong preference for the formation of aDMA. Preferentially methylates arginyl residues present in a glycine and arginine-rich domain and displays...

Protein function: Arginine methyltransferase that can catalyze the formation of both omega-N monomethylarginine (MMA) and asymmetrical dimethylarginine (aDMA), with a strong preference for the formation of aDMA. Preferentially methylates arginyl residues present in a glycine and arginine-rich domain and displays...

GSK3368715 is an inhibitor of type I protein arginine methyltransferases (PRMTs, IC50s = 3.1, 162, 38, 4.7, and 39 nM for PRMT1, 3, 4, 6, and 8, respectively). It is selective for type I PRMTs over PRMT5, 7, and 9 (IC50s = >20,408, >40,000, and >15,000 nM, respectively), as well as 20 additional methyltransferases...

EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6, IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 µM). EPZ020411 shows...

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 type II or type III PRMTs nor any additional methyltransferases...