g9a

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

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.

G9a-IN-2 (Compound 7i) is an inhibitor of the histone methyltransferase G9a, with an IC50 of 0.024 μM. It can reduce the levels of H3K9me2 and induce the expression of γ-globin mRNA. G9a-IN-2 shows potential for improving Sickle Cell Disease (SCD).

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.

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

DCG066 is an inhibitor of lysine methyltransferase G9a with anticancer activity.DCG066 inhibits the proliferation of MM cells and induces iron death through the Nrf2 HO-1 pathway and can be used in the study of leukemias.

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

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].

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 .

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

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.

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.

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.

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.

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.

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.

BRD4770, a histone methyltransferase G9a inhibitor, induces cell senescence.

GA001 is a potent G9a antagonist with an IC50 of 1.32 μM. It can induce autophagy and apoptosis, and is applicable in the treatment of breast cancer.

UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 values of 15 nM and 19 nM, respectively. It is effective in inhibiting invasion and migration of TNBC cells in vitro. Additionally, UNC0638 hydrate acts as an inhibitor of EHMT1 2 and induces the expression of fetal hemoglobin (HbF) in cultures of human erythroid progenitor cells. Furthermore, it exhibits antiviral activity against FMDV (foot-and-mouth disease virus) and VSV (vesicular stomatitis virus), demonstrating remarkable potency and selectivity across various epigenetic and non-epigenetic targets.

MS-8709 is a G9a GLP PROTAC Degrader (DC50(G9a) = 274 nM; DC50(GLP) = 260 nM) that induces G9a GLP degradation in a concentration-, time-, and ubiquitin-proteasome system (UPS)-dependent manner. It shows higher selectivity for G9a GLP over other methyltransferases, without affecting G9a GLP mRNA expression. In addition, MS-8709 demonstrates superior inhibition of prostate cancer, leukemia, and lung cancer cell growth compared to its parent compound, the G9a GLP inhibitor UNC0642, and possesses favorable murine pharmacokinetic properties for in vivo efficacy studies.

MS8511 (hydrochloride) is a specific covalent and irreversible inhibitor of G9a GLP, targeting the cysteine residue at the substrate binding site. It has an IC50 of 100 nM for G9a and 140 nM for GLP, with Kd values of 44 nM for G9a and 46 nM for GLP. This compound reduces intracellular H3K9me2 levels and enhances antiproliferative activity, making it useful for studying various cancers, including brain, breast, ovarian, lung, bladder cancers, melanoma, and colorectal cancer, as well as other diseases like Alzheimer's disease (AD), sickle cell disease, and Prader-Willi syndrome (PWS).

DS79932728 is an orally active inhibitor of G9a and GLP, with IC50 values of 12.6 nM and 75.7 nM, respectively. It induces the production of γ-globin, thereby increasing fetal hemoglobin (HbF) levels. In cynomolgus monkey models, DS79932728 enhances the proportion of F-reticulocytes (F-rets) and shows good oral absorption characteristics.

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.

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