CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.

CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.

MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .

MS0124 is a potent and selective G9A-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM, respectively.

Lsd1-in-20 is a potent dual inhibitor of LSD1/G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

DCG066 is a G9a inhibitor in vitro.

MS8511, a selective covalent irreversible inhibitor of G9a/GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46 nM (GLP). This compound effectively reduces cellular H3K9me2 levels and boosts antiproliferation activity, making it applicable in cancer research involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as studies on Alzheimer’s disease (AD), sickle cell disease, and Prader−Willi syndrome (PWS) [1].

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

CM-579 trihydrochloride is a first-in-class reversible and dual inhibitor of G9a and DNMT (IC50s: 16 nM, 32 nM) with potent in vitro cellular activity in a wide range of cancer cells.

Histone H3 (1-25), amide is a N-terminal peptide fragment of histone H3 that serves as a substrate for histone methyltransferases (HMTs). It can be utilized to identify the substrate for HMTs. Compared to histone H3 (15-39) and full-length histone H3, Histone H3 (1-25), amide proves to be more efficient as a substrate for HMT G9a.

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).

5WKS also known as ZINC97756584 is a biochemical. It is a G9a protein inhibitor.G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes H3K9me2, a reversible modification commonly associated with transcriptional gene silencing.5WKS can be used in the study of autoimmune diseases or tumors.

EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

RK-701, a highly selective and non-genotoxic G9a inhibitor, exhibits an IC 50 value of 23-27 nM. It selectively up-regulates HbF, γ-Globin, and BGLT3 expression while down-regulating H3K9me2 expression. Additionally, RK-701 inhibits BCL11A and ZBTB7A.

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.

BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.

BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM

WDR5-0102 is a compound that inhibits the WDR5-MLL1 interface (K dis = 7 μM, K d = 4 μM), selectively reducing MLL1 HMT activity without affecting the human H3K4 methyltransferase SETD7 or other HMTs, including G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5.

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells); exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

UNC0638 is an inhibitor of β-protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.

UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays.

Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.

CM-579 trihydrochloride, a first-in-class reversible, dual inhibitor of G9a and DNMT, exhibits potent in vitro cellular activity across a broad spectrum of cancer cells. It demonstrates inhibition with IC50 values of 16 nM for G9a and 32 nM for DNMT, respectively.

CSV0C018875 Hydrochloride is a novel G9a (EHMT2) inhibitor, binding tightly inside the active site cavity of G9a, inhibiting the activity of G9a in both enzyme and cell based assays with much lesser toxicity than BIX-0129.

UNC0224 is a selective inhibitor of G9a with a Ki of 2.6 nM and IC50 of 15 nM. UNC0224 also potently inhibits GLP with assay-dependent IC50 values of 20-58 nM.

ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP. It effectively inhibits H3K9me2 in cells, induces apoptosis in triple-negative breast cancer (TNBC) cells, and arrests the cell cycle at the G2/M phase [1].

RK-0133114, a G9a inhibitor and the R-enantiomer of RK-701, exhibits potent inhibition of G9a with an IC50 value of 3.7 μM. This compound is utilized in research focused on sickle cell disease (SCD) [1].

MS012 is a Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase (Kd = 46 ± 15 nM).

CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor with lower cytotoxicity than BIX-01294 [1].

Setin-1 is the most potent Set7 inhibitor that acts by inhibiting the KMTase G9a.

UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).