HA14-1 NEW
| Price | $39 | $62 | $89 |
| Package | 10mg | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-14 |
Product Details
| Product Name: HA14-1 | CAS No.: 65673-63-4 |
| Purity: 98% | Supply Ability: 10g |
| Release date: 2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | 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). |
| 細胞實驗 | 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) |
| 激酶實驗 | 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. |
| 體外活性 | In immunodeficient mice, HA14-1 (400 nM) does not significantly affect the growth of glioblastomas on its own. However, in vivo, HA14-1 (400 nM) enhances the efficacy of the DNA-damaging agent etoposide (2.5 mg/kg) in inhibiting the growth of glioblastomas. |
| 體內(nèi)活性 | When applied to follicular lymphoma cell lines HF1A3, HF4.9, and HF28RA, HA14-1 exhibits cytotoxicity with LC50 values of 4.5/12.6/8.1 μM, respectively. HA14-1 induces apoptosis in HL-60 cells in a dose-dependent manner through the activation of caspases. Moreover, HA14-1 triggers apoptosis in HF4.9, HF1A3, and HF28RA cells through caspase and ROS (Reactive Oxygen Species) pathways. |
| 存儲條件 | 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) |
| 關鍵字 | Bcl-2 Family | HA141 | HA14 1 | HA-14-1 | inhibit | Inhibitor | HA14-1 |
| 相關產(chǎn)品 | Gossypol (acetic acid) | (S)-(+)-Ibuprofen | Allethrin | Navitoclax | Docetaxel trihydrate | Gossypol | Triacetylresveratrol | Diphenyl disulfide | Lisaftoclax | Venetoclax | (E)-Ferulic acid | Thymoquinone |
| 相關庫 | 銅死亡化合物庫 | 細胞凋亡化合物庫 | 經(jīng)典已知活性庫 | 毒性化合物庫 | 抑制劑庫 | NO PAINS 化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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