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PRMTs Protein arginine methyltransferases

Inhibitors

Cat.No.  Name Information
M10637 GSK3368715 2HCl GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively.
M10495 AMI-1 disodium salt AMI-1 is a potent and selective, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50 values of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 is also a potent scavenger of NADPH-oxidase-derived superoxide.
M10073 HLCL-61 hydrochloride HLCL-61 hydrochloride is a potent and selective, first-in-class protein arginine methyltransferase 5 (PRMT5) inhibitor.
M9789 MS049 MS049 is a potent and selective inhibitor of PRMT4,6 with IC50 values of 34 nM and 43 nM, respectively.
M9420 GSK3326595 GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.
M9003 MS023 MS023 is a potent and selective, cell-active inhibitor of type I PRMTs with IC50s of 4-119 nM.
M8649 GSK591 GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.
M8561 DS-437 DS-437 is an analog of S-adenosyl methionine (SAM ), which inhibits protein arginine methyltransferases PRMT5 and PRMT7 (IC50 5.
M8379 CID 5380390 CID 5380390 is a selective inhibitor of Protein Arginine Methyltransferases PRMT1 and PRMT8.
M7456 UNC 2327 UNC 2327 is a allosteric inhibitor of PRMT3.
M7365 TC-E 5003 Tc-e 5003 is a selective inhibitor of PRMT1 with an IC50 of 1.5 µM against hPRMT1. Tc-e 5003 has anti-inflammatory properties in TLR4 signal transduction.
M6737 Furamidine dihydrochloride Furamidine dihydrochloride is a selective PRMT1 inhibitor.
M6312 LLY-283 LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.
M6142 XY1 XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive.
M5229 EPZ020411 EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has >10 fold selectivity for PRMT6 over PRMT1 and PRMT8.
M5163 SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
M4954 EPZ015666 EPZ015666 is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
M3783 C7280948 C7280948 is an inhibitor of histone arginine methyltransferase PRMT1 with IC50 values of 12.75 uM.



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