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G9a/GLP

Isoform-selective Products

G9a/GLP Products

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  • G9a/GLP Inhibitors (9)
  • New G9a/GLP Products
Catalog No. Product Name Information Product Use Citations Product Validations
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.
Acta Pharm Sin B, 2024, 14(3):1187-1203
Cell Commun Signal, 2024, 22(1):402
Dev Cell, 2023, 58(6):506-521.e5
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).
PeerJ, 2024, 12:e17222
Asian Pac J Trop Bio, 2023;, 13(6): 268-276
Cancer Cell, 2023, 41(6):1118-1133.e12
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.
Cell Rep, 2024, 43(2):113779
Cell Rep, 2023, 42(6):112566
Genome Instability & Disease , 2023, 4:21–37
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.
PLoS Biol, 2024, 22(3):e3002240
Cell Rep, 2024, 43(1):113575
Research (Wash D C), 2023, 6:0264
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.
S2943 BRD9539 BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.
E1607New 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. RK-701 treatment induces fetal globin expression in human erythroid cells and in mice and plays an essential role in γ-globin induction. RK-701 is used in the research of sickle cell disease.
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.
Acta Pharm Sin B, 2024, 14(3):1187-1203
Cell Commun Signal, 2024, 22(1):402
Dev Cell, 2023, 58(6):506-521.e5
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).
PeerJ, 2024, 12:e17222
Asian Pac J Trop Bio, 2023;, 13(6): 268-276
Cancer Cell, 2023, 41(6):1118-1133.e12
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.
Cell Rep, 2024, 43(2):113779
Cell Rep, 2023, 42(6):112566
Genome Instability & Disease , 2023, 4:21–37
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.
PLoS Biol, 2024, 22(3):e3002240
Cell Rep, 2024, 43(1):113575
Research (Wash D C), 2023, 6:0264
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.
S2943 BRD9539 BRD9539 is a histone methyltransferase G9a inhibitor, which also inhibits PRC2 activity.
E1607New 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. RK-701 treatment induces fetal globin expression in human erythroid cells and in mice and plays an essential role in γ-globin induction. RK-701 is used in the research of sickle cell disease.
E1607New 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. RK-701 treatment induces fetal globin expression in human erythroid cells and in mice and plays an essential role in γ-globin induction. RK-701 is used in the research of sickle cell disease.

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