g9a

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.

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.

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.

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

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

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

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

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

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) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

PROTACG9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with a DC50 of 336 nM for G9a and 988 nM for GLP. It exhibits inhibitory activity against G9a with an IC50 of 98 nM. This compound effectively inhibits the migration of breast cancer MCF-7 cells without affecting their proliferation and is utilized in breast cancer research.

G9a-IN-3 (compound 16g) is a potent G9a inhibitor with an IC50 of 0.002 μM. It is applicable for research in sickle cell disease.

G9a-IN-4 is a specific inhibitor of G9a with an IC50 of 32 nM. It exhibits high selectivity against other tested lysine/arginine methyltransferases. G9a-IN-4 shows enhanced enzymatic activity and demonstrates stronger antiproliferative effects on all tested cancer cell lines. It significantly inhibits H3K9me2 levels and induces autophagy via ROS generation, leading to apoptosis and G0/G1 cell cycle arrest in CT26 colon cancer cells. G9a-IN-4 is applicable for colon cancer research.

GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective inhibitor that penetrates the blood-brain barrier, targeting G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP-competitive, IC50: 0.8 μM). It acts as a potent H3K9me2 inhibitor, facilitating chromatin remodeling and reducing tau protein phosphorylation and Aβ aggregation. Additionally, GSK-3β/G9a-IN-1 inhibits the glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor, and upregulates SAGA complex members such as Eny2 and Sgf29. This compound significantly enhances memory, restores social behavior, and increases synaptic complexity in late-onset Alzheimer's disease.

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).

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

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 .

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.

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