化合物 HA14-1|T1980|TargetMol

HA14-1
65673-63-4

￥188 5mg 起订

￥325 10mg 起订

￥552 25mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 HA14-1

英文名称：: HA14-1

CAS号：: 65673-63-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98%

产品类别：: 抑制剂

货号：: T1980

Product Introduction

Bioactivity

名称	HA14-1
描述	HA14-1, a Bcl-2/Bcl-XL antagonist, is a non-peptidic ligand of a Bcl-2 surface pocket (IC50: ~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 \| Shipping with blue ice.
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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HA14-1|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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