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).

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

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 .

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.

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

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.

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.

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.

W4022 (compound 16) is an efficient dual inhibitor of the lysine methyltransferases G9a NSD2, with IC50 values of 0.241 μM for G9a and 0.017 μM for NSD2. It exhibits potent antiproliferative properties, including the ability to suppress colony formation, induce apoptosis, and inhibit metastasis of cancer cells. W4022 effectively curtails the catalytic activities of G9a and NSD2 within cells and demonstrates significant antitumor efficacy in PANC-1 xenograft models.

G9D-4 is an effective degrader of G9a with a DC50 value of 0.1 μM in PANC-1 cells, and it does not directly interfere with GLP proteins (DC50 greater than 10 μM). This compound plays a significant role in pancreatic cancer research.

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.

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.

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.

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.

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

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, a histone methyltransferase G9a inhibitor, induces cell senescence.

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.

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