CM-272 |
Catalog No.GC12367 |
CM-272는 항종양 활성을 가진 동급 최초의 강력하고 선택적인 기질 경쟁적이고 가역적인 이중 G9a/DNA 메틸트랜스퍼라제(DNMT) 억제제입니다. CM-272는 각각 8nM, 382nM, 85nM, 1200nM 및 2nM의 IC50으로 G9a, DNMT1, DNMT3A, DNMT3B 및 GLP를 억제합니다. CM-272는 세포 증식을 억제하고 세포 사멸을 촉진하여 IFN-자극 유전자 및 면역원성 세포 사멸을 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1846570-31-7
Sample solution is provided at 25 µL, 10mM.
CM-272 is a first-in-class reversible dual inhibitor against G9a and DNMTs with IC50 values of 8 nM and 382 nM, respectively [1].
G9a is a histone methyltransferase that is overexpressed in many tumors. Inhibition of G9a expression reduces cancer cell proliferation, delays disease progression and inhibits tumor metastasis. G9a interacts with DNA methyltransferase-1 (DNMT1) to coordinate DNA and histone methylation during cell division promoting transcriptional silencing of target genes. Reduction of both DNA and H3K9 methylation levels leads to reactivation of tumor suppressor genes and inhibits cancer cell proliferation [1].
CM-272 is a first-in-class reversible and substrate-competitive dual inhibitor of G9a and DNMTs. In ALL, AML and DLBCL-derived cell lines, CM-272 reduced DNA methylation in the promoter region of specific tumor suppressor genes. CM-272 also inhibited cell proliferation, blocked cell cycle progression and induced apoptosis in a dose-dependent way [1].
In immunodeficient Rag2-/-γc-/- mice injected i.v. with ALL-derived CEMO cells, CM-272 significantly increased overall survival (OS) in mice (median OS; 92±5.7 days versus 55±10.5 days; P=0.0009) without significant weight loss. In immunodeficient Rag2-/-γc-/- mice injected i.v. with AML-derived MV4-11 cells, CM-272 also prolonged OS in mice. CM-272 exerted a potent anti-tumour activity in vivo against different types of haematological malignancies by inhibiting the methyltransferase activity of both G9a/GLP and DNMTs [1].
Reference:
[1]. 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 malignancies. Nat Commun. 2017 May 26;8:15424. doi: 10.1038/ncomms15424.
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(Based on Reviews and 2 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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