Histone Methyltransferase
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COMT inhibitor
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor.
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EZH2 抑制剂
GSK126是一种有效的，高选择性的，具有S-腺苷甲硫氨酸竞争性的小分子EZH2甲基转移酶活性抑制剂，可降低总体H3K27me3水平并重新激活沉默的PRC2目标基因。
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- Lucy E. Dawson, .et al. Induction of Myogenic Differentiation Improves Chemosensitivity of Chemoresistant Cells in Soft-Tissue Sarcoma Cell Lines, Sarcoma, 2020, 2020: 8647981 PMID: 32300280
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Dupret B, .et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218
- Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
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Wdr5-MLL interaction antagonist
OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation .
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COMT inhibitor
Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.
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SMYD3 inhibitor
SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM.
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G9a/DNMT inhibitor
CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
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G9a/DNMT 抑制剂
CM-272是血液恶性肿瘤中针对G9a和DNMT的可逆双重小分子抑制剂。
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EZH2 抑制剂
3 Deazaneplanocin A(DZNep)是3-deazaadenosine的环戊烯基类似物，最初是作为S-腺苷L-homocysteine水解酶的抑制剂合成的。
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5-HT1A receptor antagonist/COMT inhibitor
Flopropione是5-HT1A受体拮抗剂，也是儿茶酚-邻甲基转移酶（COMT）抑制剂。
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EZH2/EZH1 抑制剂
UNC-1999是生物可利用抑制剂，对野生型和突变型ezh2以及ezh1具有高体外效力，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。
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- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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EZH2 抑制剂
CPI-169是一种有效的选择性EZH2抑制剂，对EZH2 WT，EZH2 Y641N和EZH1的IC50分别为0.24 nM，0.51 nM和6.1 nM。
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EZH2 抑制剂
CPI-360是一种有效的，选择性的且具有SAM竞争性的EZH2抑制剂，IC50为102.3 nM，选择性是其他甲基转移酶的100倍以上。
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EZH2 抑制剂
GSK-503是一种有效的EZH2抑制剂，具有潜在的抗癌活性。
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EZH2 抑制剂
EPZ011989是一种有效的，选择性的生物利用型EZH2抑制剂，对于EZH2 wt和EZH2 Y646，Ki <3 nM；选择性是EZH1的15倍，选择性是其他HMTase的3000倍。
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