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CM-272

CAS No. : 1846570-31-7

MCE 站：CM-272

产品活性：CM-272 是一种一流的，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。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Histone Methyltransferase  |  DNA Methyltransferase  |  Apoptosis

In Vitro: CM-272 (100-1000 nM; 12-72?hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment inhibits cell proliferation in a dose- and time-dependent manner.
CM-272 (100-1000 nM; 24?hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment blocks cell cycle progression.
CM-272 (100-1000 nM; 12-72?hours; CEMO-1, MV4-11 and OCI-Ly10 cell lines) treatment induces apoptosis in ALL, AML and DLBCL cell lines in a dose- and time-dependent manner.
CM-272 after 48?h of treatment CEMO-1 acute lymphoblastic leukaemia (ALL) cell line, MV4-11 acute myeloid leukaemia (AML) cell line and OCI-Ly10 diffuse large B-cell lymphoma (DLBCL) cell line, the GI₅₀ values of 218 nM, 269 nM and 455 nM, respectively, and is associated with a decrease in global levels of H3K9me2 and 5mC.
The therapeutic activity of CM-272 relies on the early activation of the type I IFN response in tumour cells, potentially leading to the induction of cell autonomous immunogenic death in tumour cells.

In Vivo: CM-272 (2.5 mg/kg; intravenous injection; daily; for 28 days; female Rag2^?/?γc^?/? mice) treatment significantly prolongs survival of CEMO-1 cells xenogeneic models.

相关产品：Apoptosis Compound Library  |  Reprogramming Compound Library  |  Anti-Cancer Compound Library  |  Epigenetics Compound Library  |  Bioactive Compound Library Plus  |  Histone Modification Research Compound Library  |  MG-132  |  LY294002  |  Actinomycin D  |  Mitomycin C  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  SP600125  |  Sorafenib  |  Angiotensin II human  |  MK-2206 dihydrochloride  |  5-Fluorouracil  |  Trametinib  |  Tamoxifen  |  Bortezomib  |  Gemcitabine  |  Pexidartinib  |  Acetylcysteine  |  Decitabine  |  BAY 11-7082  |  2-Deoxy-D-glucose  |  Docetaxel  |  Verteporfin  |  Temozolomide  |  Dasatinib  |  Ruxolitinib  |  Etoposide  |  GSK126

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