化合物CPI455 T3552

Product Introduction
Bioactivity


英文名: CPI-455

描述: CPI-455 是一种特异性的泛KDM5抑制剂，对 KDM5A 的IC50为 10 nM。它介导 KDM5 抑制，提高 H3K4me3 的整体水平，有抗肿瘤作用。

细胞实验: All cell lines were treated with DMSO, CPI-4203 or CPI-455 for 5 d with two changes of medium and drug. Thereafter, the cells (PC9, Colo205, Hs888, M14, SKBR3 and EVSA-T) were plated at 2×105 cells in six-well plates in triplicate and treated for an additional 9-15 d, depending on the cell line model. The Incucyte HD imaging system was used to monitor numbers of drug-tolerant cells after cells were stained with Nuclear-ID Red stain. (Only for Reference)

体外活性: CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1]. CPI-455 has a high measured affinity for the target KDM5 proteins. Within 24 hours, CPI-455 and CPI-766 can dose-dependently increases in H3K4me3, but not H3K4me2. IC50 calculation for KDM5 Inhibitor CPI-455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 5.63 mg/mL (20.21 mM)


关键字: CPI-455 | Histone Demethylase | CPI455 | CPI 455 | Inhibitor | inhibit

相关产品: KDM5-C70 | LSD1-UM-109 | GSK-LSD1 dihydrochloride | Procaine | T-3775440 hydrochloride | S2101 | JQKD82 trihydrochloride | 5-Hydroxy-7-acetoxy-8-methoxyflavone | GSK-J4 Hydrochloride | T-448 free base

相关库: Anti-Aging Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Methylation Compound Library | NO PAINS Compound Library | Chromatin Modification Compound Library

化合物CPI455 T3552信息由TargetMol中国为您提供，如您想了解更多关于化合物CPI455 T3552报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途