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.

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).

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).

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.

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-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).

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.

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).

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].

Amino-PEG9-alcohol is a PEG-based linker for PROTACs [Proteolysis Targeting Chimeras], facilitating the conjugation of two essential ligands for PROTAC formation and enabling selective protein degradation via the ubiquitin-proteasome system within cells.

Azido-PEG9-alcohol, a PEG-based PROTAC linker, is utilized in PROTAC synthesis.