EZM2302 (GSK3359088) is the first potent and selective inhibitor of CARM1 enzymatic activity that exhibits anti-proliferative effects both in vitro and in vivo,in biochemical assays (IC50=6nM) with broad selectivity against histone methyltransferases.

Furamidine dihydrochloride (NSC 305831) tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM.

Gambogenic acid (GNA) is a polyprenylated xanthone isolated from gamboge, shows potent antitumor activity and can effectively inhibit the survival and proliferation of cancer cells.

GNA002 (GNA-002) is a gambogenic acid (GNA) derivative that specifically and covalently binds to Cys668 within the EZH2-SET domain, trigges EZH2 degradation (IC50=1.1 uM) through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.

GSK-2807 (GSK 2807, GSK2807) is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki of 14 nM.

GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

GSK503 is a specific EZH2 methyltransferase inhibitor.

HLCL-61 is a first-in-class small-molecule inhibitor of PRMT5 for treatment of acute myeloid leukemia.

JQEZ5 is a novel and potent EZH2 inhibitor.

LLY-507 is a chemical probe for SMYD2 (a protein lysine methyltransferase).

MAK683 is a novel PRC2/EED inhibitor.

MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-MLL interaction.

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.

MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.

MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 that is active in cells.

Negative control of SGC 707. Exhibits >3000-fold lower potency (IC50 >100 μM) compared to the active analog.

OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM).

OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model.