GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.

TACH101 (QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of <0.1 uM against all four isoforms.TACH101 demonstrated potent increase of H3K36me3 levels (EC50 <0.001 uM, HTRF) in KYSE-150 cell line engineered to overexpress KDM4C and showed potent anti-proliferative activity in multiple cell lines in OncoPanel.Sub-micromolar levels of TACH101 induced apoptosis in human colorectal (HT-29), esophageal (KYSE-150), and triple negative breast cancer (MDA-MB-231) cell lines with EC50s of 0.033-0.092 uM.TACH101 triggered effective tumor growth control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.

SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.

Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro.

UBCS385 (Sirt4 inhibitor 60) is a potent, selective inhibitor of mitochondrial deacylase Sirtuin 4 (Sirt4) with IC50 of 0.9 uM.

UBCS373 (Sirt4 inhibitor 69) is a highly isoform selective inhibitor of mitochondrial deacylase Sirtuin 4 (Sirt4) with IC50 of 16 uM.

SirReal1.1 is a potent, selective inhibitor of Sirtuin 2 (Sirt2) with IC50 of 0.16 uM.

SCIC2.1 is a potent small molecule SIRT1 activator (175%, AC50=36.8 uM), directly binds SIRT1 and protects SIRT1 from thermal degradation.

MC3482 is a potent, specific SIRT5 inhibitor, increases the ammonia content in cells leading to autophagy and mitophagy, shows selective SIRT5 inhibition vs SIRT1-3..

MC3138 is a potent and selective small-molecule SIRT5 activator, inhibits proliferation in SIRT5-low PDAC cell lines and organoids.

MC 2494 is a nove potent, pan-Sirtuin (SirT) inhibitor, increases RIP1 acetylation in the death domain and induces bona fide tumour-restricted acetylated RIP1/caspase-8-mediated apoptosis.

FLS-359 (FLS-359) is a selective, allosteric inhibitor of sirtuin 2 (SIRT2) deacetylase activity with IC50 of 3 uM, shows no activity against SIRT1 and SIRT3, exhibits broad-spectrum antiviral activity.

40569Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.

2800Z is a specific SIRT7 inhibitor, significantly inhibits SIRT7 deacetylation activity without effects on SIRT1 and SIRT6 activities, induces apoptosis and increases chemosensitivity to sorafenib in human liver cancer.

UNC9512 is a selective methyl-lysine reader p53 binding protein 1 (53BP1) antagonist, binds the 53BP1 tandem Tudor domain (TTD) with TR-FRET IC50 of 0.46 uM, and SPR/ITC Kd vfalues of 0.17/0.41 uM respectively.

UNC7648 is a small molecule inhibitor of the methyl-lysine reader p53 binding protein 1 (53BP1) tandem Tudor domain (TTD) with TR-FRET IC50 of 8.6 uM.

SKLB-03220 (SKLB03220) is a potent, selective EZH2 covalent inhibitor with IC50 of 1.72 nM (EZH2 WT).

(R,R)-59 is a small-molecule ligand activator for methyltransferase SETDB1 Triple Tudor Domain (3TD reader domain) with binding IC50 of 1.2 uM in TR-FRET assays, specifically promotes in vitro SETDB1-mediated methylation of lysine 64 of protein kinase Akt

PRT543 is a highly potent, selective and SAM cpmpetitive inhibitor of protein arginine methyltransferase 5 (PRMT5) with IC50 of 10.8 nM.

PRT382 (PRT-382) is a potent, selective and SAM-competitive PRMT5 inhibitor with IC50 of 2.8 nM in filtration binding assays with recombinant human PRMT5/MEP50 and histone H2A as the protein substrate.

A first-in-class, potent and selective inhibitor of SETD7 methyltransferase with Ki app/IC50 of 0.33/2 nM.

PF-06821497 S enantiomer is a novel potent, selective, orally bioavailable EZH2 inhibitor with Ki of <0.1 and 1.15 nM aginast both wt and mutant Y641N EZH2, respectively.

MS1262 is a highly potent, selective and brain-penetrant inhibitor of G9a/GLP methylase with IC50 of 19/6 nM, respectively.

A potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50 of 34±10 nM and 43±7 nM, respectively.

M-808 (M808) is a highly potent, selective and covalent inhibitor of menin-MLL interaction with binding IC50 of 2.6 nM, forms a covalent bond with Cys329 in menin.

KTX-1001 is a potent, selective histone methyltransferase NSD2 (WHSC1, MMSET) inhibitor targeting the catalytic SET domain.

KMI169 (KMI-169) is a potent and selective lysine methyltransferase 9 (KMT9) inhibitor with ITC Kd of 25 nM and enzymatic IC50 of 50 nM.

JS1310 (JS-1310) is a specific small-molecule PRMT7 inhibitor with IC50 of 5 uM (human PRMT7), displays no acitivity against type I PRMTs (PRMT1, 3, 4, 6, and 8, IC50 >100 uM) or the type II PRMT5 (IC50=50 uM).

iPRMT1 is a potent and selective PRMT1 inhibitor with IC50 of 270 nM, shows good selectivity over other PRMTs.

HKMTI-1-005 is a potent, substrate-competitive dual inhibitor of EZH2 and the closely related G9A/GLP H3K9 methyltransferases with IC50 of 0.1 uM (EHMT2).