CM-272
Cat. No.：YN270039
CAS No. ：1846570-31-7
| 产品名称: | CM-272 |
| CAS No.: | 1846570-31-7 |
| Chemical Name: | 6-methoxy-2-(5-methyl-2-furanyl)-N-(1-methyl-4-piperidinyl)-7-[3-(1-pyrrolidinyl)propoxy]-4-quinolinamine |
| Synonyms: | 6-methoxy-2-(5-methyl-2-furyl)-N-(1-methyl-4-piperidyl)-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-amine;6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinolin-4-amine;6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpip |
| 分子量: | 478.63 |
| 分子式: | C₂₈H₃₈N₄O₃ |
| SMILES: | CN(CC1)CCC1NC2=CC(C3=CC=C(C)O3)=NC4=CC(OCCCN5CCCC5)=C(OC)C=C42 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | CM-272 是一种首创的，有效的，选择性的，底物竞争性的且可逆的双重G9a/DNA 甲基转移酶 (DNMTs) 抑制剂。CM-272 抑制G9a，DNMT1，DNMT3A，DNMT3B和GLP，IC50分别为 8 nM，382 nM，85 nM，1200 nM 和 2 nM。CM-272 抑制细胞增殖并促进细胞凋亡，诱导干扰素刺激的基因和免疫原性细胞死亡。抗肿瘤活性。 |
| IC50和靶点: | [{name:"G9a:8 nM (IC50)"},{name: "EHMT1/GLP/KMT1D:2 nM (IC50)"},{name: "DNMT1:382 nM (IC50)"},{name: "DNMT3A:85 nM (IC50)"},{name: "DNMT3B:1200 nM (IC50)"}] |
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San José-Enériz, E., Agirre, X., Rabal, O., et al.Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignanciesNat. Commun.8,15424(2017)
Rabal, O., San José-Enériz, E., Agirre, X., et al.Discovery of reversible DNA methyltransferase and lysine methyltransferase G9a inhibitors with antitumoral in vivo efficacyJ. Med. Chem.61(15),6518-6545(2018)
Colyn, L., Bárcena-Varela, M., Álvarez-Sola, G., et al.Dual targeting of G9a and DNMT1 for the treatment of experimental cholangiocarcinomaHepatology,(2020)
Segovia, C., San José-Enériz, E., Munera-Maravilla, E., et al.Inhibition of a G9a/DNMT network triggers immune-mediated bladder cancer regressionNat. Med.25(7),1073-1081(2019)
