NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2.

AH237 (AH-237) is a potent and selective inhibitor for PRMT4 and PRMT5 with IC50 of 2.8 and 0.42 nM, respectively.AH237 (AH-237) displayed over 50-fold selectivity against a panel of 41 MTases such as PRMTs, PKMTs, NTMT1/2, and DNA methyltransferases (DNMTs), Its potency was also confirmed for PRMT1 (IC50 = 5.9 uM) and PRMT7 (IC50 = 831 nM).

ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.AS-99 strongly bind to the ASH1L SET domain with Kd values of 0.89 uM.AS-99 displayed no significant inhibition (>100-fold selectivity) at 50 uM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2.AS-99 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations with the GI50 values of 1.8-3.6 uM, showed a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, without toxicity in normal cells.AS-99 impairs transcriptional program of MLL fusion proteins and reduces leukemia burden.AS-99 reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.

BAY-155 (BAY155) is a novel, potent and selective menin-MLL inhibitor with binding IC50 of 8 nM, 10-fold better compared to that of MI-503; BAY-155 demonstrated a significantly enhanced selectivity profile compared to MI-503 in a panel of assays covering numerous safety pharmacology-relevant targets including GPCRs, ion channels and transporters. BAY-155 shows anti-proliferative activity in a large cell line panel, exhibits specific therapeutic activityin AML/ALL models.

BR-001 (BR001) is a potent, selective, allosteric inhibitor of EED subunit of PRC2 complex, disrupts EED-H3K27me3 interaction (IC50=4.5 nM).BR-001 directly binds to EED in the H3K27me3-binding pocket, BR-001 significantly increases the thermal stability of EED in thermal shift assay.BR-001 is selective for EED, has no activity against 371 wild-type kinases.BR-001 significantly reduced the cellular H3K27me3 level and also exhibited a strong antiproliferative effect in Karpas 422 cells.BR-001 inhibited proliferation of DLBCL cells and tumor growth, and upregulated target genes expression.BR-001 has potent antitumor efficacy in vivo, modulates immune response to suppress syngeneic CT26 colon tumor.

DC541 (DC 541) is a potent, selective peptidomimetic inhibitor of Protein N-terminal methyltransferase NTMT1 with IC50 of 0.34 uM; DC541 exhibits over 300-fold selectivity to several methyltransferases. DC541 inhibited funtions the cellular α-N-terminal methylation level of regulator of chromosome condensation 1 (RCC1, IC50 value of 30 μM) in human colorectal cancer HT29 cells.

MU1656 (MU 1656 ) is a potent, highly selective inhibitor of histone methyltransferase DOT1L with IC50 of 2 nM; MU1656 displays highly selectively against a panel of 37 methyltransferases. MU1656 is more metabolically stable and significantly less toxic in vivo than pinometostat.

NAH-C3-GPKK is a potent, selective protein N-terminal methyltransferase 1 (NTMT1) bisubstrate inhibitor with Kiapp of 7 nM in endogenous proteomes.NAH-C3-GPKK also potently inhibit a methyltransferase complex HemK2-Trm112 (also known as KMT9-Trm112, IC50=0.3 uM).NAH-C3-GPKK is the first potent inhibitor for HemK2/KMT9.

OR-S0 is a potent, selective EZH2 inhibitor with IC50 of 11 nM, weakly inhibitor EZH1 (IC50=91 nM).OR-S0 inhibits H3K27me3 in HCT116 cells with IC50 of 24 nM, inhibited the growth of KARPAS‐422 cells in a dose‐dependent manner with GI50 of 210 nM.

PFI-5 a highly biochemically potent, selective, and cell-active SMYD2 chemical probe with IC50 of 8 nM.PFI-5 inhibits p53 methylation in MCF7 cells with EC50 of 1.3 uM, with no toxicity.

PRC2 EED-IN-1 is a potent, selective, allosteric, orally bioavailable inhibitor of the EED subunit of histone methyltransferase PRC2 with IC50 of 44 nM (H3K27me3 inhibition).PRC2 EED-IN-1 retains efficacy against EZH2 inhibitor-resistant cell lines (Karpas 44 cell IC50=27 nM), exhibits in vivo efficacy in EZH2-driven tumors in vivo.

SGC3027N (SGC-3027N) is a negative control compound for SGC3027, shows markedly less potent (14 uM) against PRMT7 and other protein methyltransferases.

SGC6870 (SGC-6870 (R-isomer)) is a potent, selective, cell-active PRMT6 inhibitor with IC50 of 77 nM.SGC6870 displays outstanding selectivity for PRMT6 over a broad panel of other methyltransferases and nonepigenetic targets.SGC6870 binds to a unique, induced allosteric pocket of PRMT6.SGC6870 engages PRMT6 and potently inhibits its methyltransferase activity in cells.SGC6870 is a well-characterized PRMT6 chemical probe and a valuable tool for further investigating PRMT6 functions in health and disease.

SGC6870N is the negative control of SGC-6870 (R-isomer), which is a potent, selective, cell-active PRMT6 inhibitor.

SGC8158 (SGC-8158) is a potent, selective, and SAM-competitive inhibitor of PRMT7 with IC50 of <2.5 nM, the active component of it's cell permeable prodrug SGC3027.

SKI-73 is a CARM1 chemical probe with pro-drug properties, can readily penetrate cell membranes and then be processed into two active CARM1 inhibitors.SKI-73 (10 uM) fully suppresses the methylation of BAF155 Arg1064 in MCF-7 cells.SKI-73 inhibits in vitro invasion but not proliferation of breast cancer cells ( MDA-MB-231 cell, EC50=1.3 uM).SKI-73 recapitulates the anti-invasion effect of the genetic perturbation of CARM1.Either CARM1 knockout or CARM1 inhibition with SKI-73 alters the epigenetic plasticity in a proliferation-independent manner by replacing the most invasion-prone subpopulation with the non-invasive subpopulation(s) to suppress the invasive phenotype.

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells.

SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 11.7 nM.SMYD3 inhibitor 29 exhibits high potency by inhibiting SMYD3's enzymatic activity and showing antiproliferative activity against HepG2 in 3D cell culture (GI50=1.04 uM).SMYD3 inhibitor 29 inhibits cellular MAP3K2 methylation.SMYD3 inhibitor 29 displayed high selectivity when tested against a panel of methyltransferases, namely, SMYD1-2, G9a, PRDM9, and PRMT5.

SW2_152F (SW2 152F) is a potent, selective, cell permeable CBX2 chromodomain probe, binds to the N-terminal chromodomain (ChD) with Kd of 80 nM.SW2_152F displays 24-1,000-fold selectivity for CBX2 ChD over other CBX paralogs (CBX4/6/7/8) in vitro.SW2_152F is cell permeable, selectively inhibits CBX2 chromatin binding in cells, and blocks neuroendocrine differentiation of prostate cancer cell lines in response to androgen deprivation.

TC-5115 (TC5115 ) is a potent, selective inhibitor of MLL1 SET domain with IC50 of 15 nM, 48 times more potent than the pan-methyltransferase inhibitor SAH.

TDI-11904 is a highly potent, and peripherally active EZH2 inhibitor.

TDI-6118 is a potent, selective brain-penetrant EZH2 inhibitor with IC50 of 14 nM, inhibits cellular H3K27me with IC50 of 580 nM.