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Cat. No. Product Name CAS No. Information
PC-35520

PF-06855800

1989620-04-3

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.

PC-63461

LLY-283

2040291-27-6

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).

PC-43301

EPZ020411 hydrochloride

2070015-25-5

EPZ020411 is a potent, selective PRMT6 inhibitor with IC50 of 10 nM, displays 10-fold and 20-fold selectivity over PRMT1/8, and >100-fold over other histone methyltransferases (PRMT3/4/5/7); dose-dependently decreases H3R2 methylation A375 cell line with IC50 of 0.637 uM, with no affect levels of PRMT6 expression; exhibits good bioavailability following subcutaneous dosing in rats making it a suitable tool for potential in vivo target validation studies.

PC-61791

PR5-LL-CM01

1005307-86-7

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.

PC-61209

EPZ 025654

1888328-89-9

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

PC-61030

EZM 2302

1628830-21-6

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.

PC-60423

A-893

1868232-32-9

A-893 (A893) is a potent, selective and cell active lysine methyltransferase SMYD2 inhibitor with IC50 of 2.8 nM; displays high selectivity against a panel of 31 other methyltransferases (<50% inhibition at 1 uM); reduces p53K370me1 without effects on overall p53 levels in A549 p53 cellular assay, has unexpectedly notable improvement in potency (>80-fold) compared with AZ-505 .

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