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Cat. No. Product Name CAS No. Information


PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM; demonstrates antiproliferative activity in Z-138 cancer cells with IC50 of 1 nM, also shows anti-tumor activity in Z-138 mice xenograft models.




LLY-283 (LLY283) is a potent, selective inhibitor of arginine methyltransferase 5 (PRMT5) with IC50 of 22 nM; displays excellent against other arginine methyltransferases including the closely related PRMT7 and the type II PRMTs such as PRMT4 and 6; decreases SmBB’-Rme2s levels in MCF7 cells with IC50 of 25 nM, also inhibits the PRMT5 mediated regulation of the splicing of MDM4; inhibits proliferation of A375 cells with IC50 of 45.6 nM; inhibits Tumor growth in mouse xenograft (A375, 20 mg/kg; QD).




PR5-LL-CM01 is a novel selective, small-molecule inhibitor of PRMT5 methyltransferase with IC50 of 7.5 uM; displays >10-fold selectivity over PRMT3, and no inhibitory activity over PRMT1/4/6/8; exhibits cell viability inhibition with IC50 of 2-4 uM in PDAC cells, IC50 of 10-11 uM in CRC cells, more potent than EPZ015666; significantly inhibits NF-κB activation in PDAC and CRC cells, and shows dramatic anti-tumor efficacy in vivo.


EPZ 025654


EPZ025654 (GSK 35336023) is a potent, selective arginine methyltransferase CARM1 inhibitor with IC50 of 3 nM.


EZM 2302


EZM 2302 (EZM2302, GSK 3359088) is a potent, selective, orally available arginine methyltransferase CARM1 inhibitor with IC50 of 6 nM, with broad selectivity against other HMTases; demonstrates in vitro anti-proliferative activity consistent with specific methyl mark inhibition with IC50 of <100 nM in 9/15 multiple myeloma cell lines, decreases methylation of PABP1 (IC50 =38 nM) and SmB (IC50=18 nM); displays dose-dependent inhibition of CARM1 substrate methylation in vivo, and induces growth inhibition of human multiple myeloma tumor xenografts in mice.




GSK-2807 (GSK 2807, GSK2807) is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki of 14 nM; displays 24-fold selectivity over SMYD2, and a panel of PRMTs including: PRMT1, PRMT4, PRMT5, NSD2, NSD3, DOT1L, G9a, and ASH1L.




BCI-121 (BCI121) is a substrate-competitive SMYD3 inhibitor that significantly inhibits SMYD3-substrate interaction and chromatin recruitment and is effective in reducing proliferation in various cancer cells types; impairs SMYD3-mediated H4 in vitro methylation, reduced proliferation of HT29 and HCT116 cells; reproduces the effects of SMYD3-targeted RNAi.

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