KDOAM-25 citrate 是有效，高选择性的 KDM5 抑制剂，对 KDM5A，KDM5B，KDM5C，KDM5D 的 IC50 分别为 71 nM，19 nM，69 nM，69 nM。KDOAM-25 citrate 可增加转录起始位点的整体 H3K4 甲基化，并损害多发性骨髓瘤 MM1S 细胞的增殖。
货号:ajcx15204
CAS:N/A
分子式:C21H33N5O9
分子量：499.51
溶解度:DMSO: 200 mg/mL (400.39 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KDOAM-25 citrate is a potent and highly selective KDM5 sub-family of histone lysine demethylases inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells[1].

[1]. Tumber A, et al. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol. 2017 Mar 16;24(3):371-380.