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CM-272
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C28H38N4O3
- MW: 478.63
Description
CM-272 is a first-in-class, potent, selective and reversible dual inhibitor of histone methyltransferase G9a (EHMT2) and DNA methyltransferase 1 (DNMT1) with IC50 values of 8 nM and 382 nM, respectively. By simultaneously targeting histone and DNA methylation pathways, CM-272 effectively modulates epigenetic regulation and gene expression.
G9a and DNMT1 are key epigenetic regulators involved in transcriptional repression, chromatin remodeling, cancer progression, and immune evasion. CM-272 inhibits cell proliferation, promotes apoptosis, induces interferon-stimulated genes, and triggers immunogenic cell death. In preclinical studies, CM-272 significantly prolonged survival in acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), and diffuse large B-cell lymphoma (DLBCL) xenograft models, making it a valuable tool for epigenetics, cancer biology, and immuno-oncology research.
Key Features
- First-in-class dual G9a and DNMT1 inhibitor
- IC50: 8 nM for G9a and 382 nM for DNMT1
- Potent and reversible epigenetic modulator
- Induces interferon-stimulated genes and immunogenic cell death
- Demonstrates antitumor activity in hematologic cancer models
Applications
- Epigenetics and chromatin biology research
- G9a and DNMT1 target validation studies
- AML, ALL and DLBCL cancer research
- Immunogenic cell death and immuno-oncology investigations
- Cancer epigenetics and transcriptional regulation studies
More Information
| Parent CAS No. | 1846570-31-7 |
|---|---|
| Chemical Name | 6-Methoxy-2-(5-methylfuran-2-yl)-N-(1-methylpiperidin-4-yl)-7-(3-(pyrrolidin-1-yl)propoxy)quinolin-4-amine |
| SMILES | C1(OC)C=C2C(NC3CCN(C)CC3)=CC(C3=CC=C(C)O3)=NC2=CC=1OCCCN1CCCC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C28H38N4O3/c1-20-7-8-26(35-20)25-18-23(29-21-9-14-31(2)15-10-21)22-17-27(33-3)28(19-24(22)30-25)34-16-6-13-32-11-4-5-12-32/h7-8,17-19,21H,4-6,9-16H2,1-3H3,(H,29,30) |
| InChiKey | RLQLKZTYUYIWDB-UHFFFAOYSA-N |
| CID | 118607432 |
| Short Description | G9a/DNMT inhibitor |
References
- E San José-Enériz et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424.
- E Rabal O, San José-Enériz et al. Discovery of Reversible DNA Methyltransferase and Lysine Methyltransferase G9a Inhibitors with Antitumoral in Vivo Efficacy. J Med Chem. 2018 Aug 9;61(15):6518-6545.
- JA Rabal O, Sánchez-Arias et al. Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces. J Med Chem. 2018 Aug 9;61(15):6546-6573.
- M Bárcena-Varela et al. Dual Targeting of Histone Methyltransferase G9a and DNA-Methyltransferase 1 for the Treatment of Experimental Hepatocellular Carcinoma. Hepatology. 2019 Feb;69(2):587-603.
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