化合物HA14-1 T1980

Product Introduction
Bioactivity


英文名: HA14-1

描述: HA14-1 是一种 Bcl-2/Bcl-xL 拮抗剂，与 Bcl-2 上的特定口袋结合，IC50约为 9 μM。

细胞实验: The cytotoxic effects of HA14-1 against different FL cell lines are determined by the MTT assay. Briefly, the cells (5000/well) are incubated in triplicate in 96-well plate in the presence or absence of HA14-1 for 20 h at 37 °C. Thereafter, the MTT solution is added to each well. After 4 h incubation at 37 °C, the optical density (OD) is measured by means of 96-well plate reader, with the extraction buffer as a blank. The following formula is used: percentage cell viability = (OD of the experiment samples/OD of the control) × 100. Sigmoidal dose-response curves are fitted to the mean cell viability plotted against log HA14-1 dose and lethal concentration 50% (LC50) values are calculated from the resulting curves using Prism 4.0 softw(Only for Reference)

激酶实验: Affinity determination: The binding affinity of organic compounds to Bcl-2 protein in vitro is determined by a competitive binding assay based on fluorescence polarization. For this assay, 5-carboxyfluorecein is coupled to the N terminus of a peptide, GQVGRQLAIIGDDINR, derived from the BH3 domain of Bak (Flu-BakBH3), which has been shown to bind to the surface pocket of the Bcl-xL protein with high-affinity. According to our molecular modeling studies and binding measurement using fluorescence polarization, the Flu-BakBH3 peptide binds the surface pocket of Bcl-2 with a similar affinity. Bcl-2 used in this assay is a recombinant GST-fused soluble protein. Flu-BakBH3 and Bcl-2 protein are mixed in the presence or absence of organic compounds under standard buffer conditions and are incubated for 30 min. The binding of Flu-BakBH3 to Bcl-2 protein is measured on a LS-50 luminescence spectrometer equipped with polarizers using a dual path length quartz cell (500 μl). The fluorophore is excited with vertical polarized light at 480 nm (excitation slit width 15 nm), and the polarization value of the emitted light is observed through vertical and horizontal polarizers at 530 nm (emission slit width 15 nm). The binding affinity of each compound for Bcl-2 protein is assessed by determining the ability of different concentrations of the compound to inhibit Flu-BakBH3 binding to Bcl-2.

体外活性: 在免疫缺陷小鼠体内,HA14-1（400 nM）对胶质母细胞瘤的生长无明显作用.但在体内HA14-1（400 nM）可增强DNA损伤剂依托泊苷（2.5 mg/kg）对胶质母细胞瘤生长的作用效果.

体内活性: 作用于滤泡性淋巴瘤细胞系HF1A3, HF4.9和HF28RA时,HA14-1具有细胞毒性,LC50为4.5/12.6/8.1 μM。通过激活caspase,HA14-1剂量依赖性诱导HL-60细胞凋亡。HA14-1经caspase和ROS诱导HF4.9,HF1A3和HF28RA细胞凋亡。

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

溶解度: Ethanol : 40.9 mg/mL (100 mM)
DMSO : 40.9 mg/mL (100 mM)


关键字: Bcl-2 Family | HA141 | HA14 1 | HA-14-1 | inhibit | Inhibitor | HA14-1

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相关库: Toxic Compound Library | Mitochondria-Targeted Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | PPI Inhibitor Library | Apoptosis Compound Library | Preclinical Compound 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