CPI-455 - KDM5 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECPI-455Cat. No.: HY-100421CAS No.: 1628208-23-0分式: CHNO分量: 278.31作靶点: Histone Demethylase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 34 mg/mL (122.17 mM)* means soluble,

2、 but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.5931 mL 17.9656 mL 35.9312 mL5 mM 0.7186 mL 3.5931 mL 7.1862 mL10 mM 0.3593 mL 1.7966 mL 3.5931 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 CPI-455种有效的特异性 KDM5 抑制剂。IC50 & Target KDM5 1体外研究CPI-455 me

3、diates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreasesthe number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEagents 1. CPI-455, with high measured affinity for the ta

4、rget KDM5 proteins. Within 24 hours, increases inH3K4me3, but not H3K4me2, are observed after exposure to either of the two active compounds, CPI-455and CPI-766, in a dosedependent manner. IC50 calculation for KDM5 Inhibitor CPI0455 in 3 luminal breastcancer cell lines MCF-7, T-47 and EFM-19 are 35.

5、4, 26.19 and 16.13 M, respectively 2.PROTOCOLCell Assay 2 MCF-7 is a luminal breast cancer cell line. MCF-7 is grown in MEM supplemented with 10% fetal bovineserum (FBS) and is incubated at 37C with a 5% CO2 atmosphere. For each treatment condition, 2.5105MCF-7 cells are plated in T25 flask and allo

6、wed to rest overnight. The following day, the media is aspiratedand replaced with media containing DAC at a final concentration of 62.5 nM. DAC media is aspirated andreplaced every 24 hours for a total treatment time of 72 hours. Following DAC treatment, media is aspiratedand replaced with media sup

7、plemented with 2% FBS containing KDM5 inhibitors (e.g., CPI-455) at a finalconcentration of 9.375 M. Cells are harvested following 72 hours of KDM5 inhibitor treatment 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cancers (Basel). 2019 J

8、an 15;11(1). pii: E92.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016Jul;12(7):531-8.2. Benjamin R. Leadem. NOVEL HISTONE DEMETHYLASE INHIBITORS SYNERGISTICALLYMcePdfHeightCaution: Product has not been fully validated for medical applications