G9a/GLP Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S7230	UNC0642	UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.	Cell Death Discov, 2025, 11(1):31 Cell Genom, 2025, 5(8):100916 FASEB Bioadv, 2025, 7(7):e70035
E7598	UNC0321	UNC0321 is a potent and selective inhibitor of G9a histone methyltransferase. It displays high potency at the picomolar level, with a Ki of 63 pM and assay-dependent IC50 values between 6-9 nM. This compound also acts as an inhibitor of GLP. It demonstrates anti-apoptotic effects and holds potential for therapeutic use in diabetic vascular complications.
S2943	BRD9539	BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.
E1607	RK-701	RK-701 is a highly selective, potent, and low-toxicity inhibitor of histone methyltransferases G9a and GLP1 with IC50 values of 23-27 nM and 53 nM. This compound treatment induces fetal globin expression in human erythroid cells and in mice and plays an essential role in γ-globin induction. It is used in the research of sickle cell disease.
S8006	BIX-01294 Trihydrochloride	BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.	Clin Transl Med, 2025, 15(1):e70164 Mol Metab, 2025, 94:102113 Acta Pharm Sin B, 2024, 14(3):1187-1203
S8068	Chaetocin	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. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).	Research (Wash D C), 2025, 8:0602 Cell Rep, 2025, 44(6):115742 Int J Mol Sci, 2024, 25(17)9215
S8071	UNC0638	UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. This compound has anti-viral activities.	bioRxiv, 2025, 2025.07.01.662447 Cell Rep, 2024, 43(2):113779 Cell Rep, 2024, 43(8):114548
S7572	A-366	A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM and 38nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.	Cell Rep, 2024, 43(1):113575 Cell Mol Life Sci, 2024, 81(1):128 Cancers (Basel), 2023, 15(8)2199
S7591	BRD4770	BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.	Adv Healthc Mater, 2024, e2401192. Hum Cell, 2023, 10.1007/s13577-023-00924-4 Cell Insight, 2023, 2(4):100112
S7020	UNC0646	UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.