化合物FX1 T4089

Product Introduction
Bioactivity


英文名: FX1

描述: FX1 是一种强效特异性BCL6抑制剂，IC50大约为 35 μM。

细胞实验: Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compared with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in a constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index [1].

动物实验: Cell viability is determined with the fluorescent redox dye. Fluorescence is determined for 3 replicates per treatment condition or vehicle with the microplate reader. Cell viability of the drug-treated cells is normalized to their vehicle-treated controls, and the results are expressed as percentage viability. The drug effect as 100-percentage viability is calculated. Through dose-effect curves the drug concentration that inhibits the growth of cell lines by 50% compare with vehicle (GI50) is determined. Experiments are performed in triplicate. For combination treatments, cells are exposed to a dose curve of each drug alone or their combination in constant ratio, and cell viability is determined. To compare different schedules of treatments, the cells are treated in triplicate as follows: FX1 and doxorubicin simultaneously and cells treated for 48 hours; FX1 first and 24 hours after doxorubicin is added and treats for an extra 48 hours; doxorubicin first and 24 hours after FX1 is added and treats for an extra 48 hours. Then, the software is used to plot dose-effect curves and calculate the dose-reduction index[1].

体外活性: FX1 markedly reduces recruitment of SMRT and BCOR to all 3 BCL6 target genes. There is little presence of SMRT at these loci in the BCL6-negative DLBCL cell line, which is not affected by FX1. After treatment with 50 μM FX1 for 6 hours, the superior potency of FX1 versus 79-6 in disrupting BCL6 binding to SMRT is evident when these small molecules are compared head to head in quantitative ChIP assays in DLBCL cells.

体内活性: Total B cell abundance is unaffected by FX1. FX1 significantly deplete GC B cells (GL7+FAS+B220+). Staining with B220 antibody reveals normal B cell follicular structures, whereas staining for the GC B cell-specific marker peanut agglutinin shows profound loss of GCs. The half-life is estimated to be approximately 12 hours. No signs of toxicity, inflammation, or infection are evident from H&E-stained sections of spleen, lung, gastrointestinal tract, kidney, heart, liver, and bone marrow of the fixed organs from mice treated with FX1 compare with the vehicle.

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

溶解度: DMSO : 25 mg/mL (67.79 mM)


关键字: inhibit | Apoptosis | Bcl-2 Family | FX-1 | FX1 | FX 1 | Inhibitor

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相关库: Mitochondria-Targeted Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | PPI Inhibitor Library | Apoptosis Compound Library | Cuproptosis Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

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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