G9a/GLP

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
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.
Cancer Metab, 2022, 10(1):4
Blood, 2021, blood.2020009195
Blood, 2021, 138(9):790-805
S7572 A-366 A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.
Pharmacol Res, 2022, 177:106122
Nat Med, 2019, 25(7):1073-1081
Genome Res, 2019, 29(10):1659-1672
S7591 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.
Pharmacol Res, 2022, 177:106122
Cancer Res, 2018, 78(20):5731-5740
Hum Pathol, 2018, 72:117-126
S8006 BIX 01294 BIX01294 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.
Pharmacol Res, 2022, 177:106122
Int J Mol Sci, 2022, 23(8)4213
Adv Sci (Weinh), 2021, e2100779
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).
Eye Vis (Lond), 2022, 9(1):4
Free Radic Biol Med, 2021, 178:147-160
Cancer Discov, 2021, candisc.0872.2020
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. UNC0638 has anti-viral activities.
PLoS Pathog, 2022, 18(5):e1010505
Adv Sci (Weinh), 2021, e2100779
Sci Adv, 2021, 7(3)eaba8053
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.
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.
Cancer Metab, 2022, 10(1):4
Blood, 2021, blood.2020009195
Blood, 2021, 138(9):790-805
S7572 A-366 A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.
Pharmacol Res, 2022, 177:106122
Nat Med, 2019, 25(7):1073-1081
Genome Res, 2019, 29(10):1659-1672
S7591 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.
Pharmacol Res, 2022, 177:106122
Cancer Res, 2018, 78(20):5731-5740
Hum Pathol, 2018, 72:117-126
S8006 BIX 01294 BIX01294 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.
Pharmacol Res, 2022, 177:106122
Int J Mol Sci, 2022, 23(8)4213
Adv Sci (Weinh), 2021, e2100779
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).
Eye Vis (Lond), 2022, 9(1):4
Free Radic Biol Med, 2021, 178:147-160
Cancer Discov, 2021, candisc.0872.2020
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. UNC0638 has anti-viral activities.
PLoS Pathog, 2022, 18(5):e1010505
Adv Sci (Weinh), 2021, e2100779
Sci Adv, 2021, 7(3)eaba8053
Tags: G9a/GLP inhibitor | G9a/GLP activator | G9a/GLP Inhibition