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  • 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸|T4371|TargetMol

6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸|T4371|TargetMol

CD437
125316-60-1
262 1mg 起订
369 2mg 起订
578 5mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸
英文名称:
CD437
CAS号:
125316-60-1
品牌:
TargetMol
产地:
美国
保存条件:
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.63%
产品类别:
抑制剂
货号:
T4371

Product Introduction

Bioactivity

名称CD437
描述CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.
细胞实验For morphological analysis, cells are treated with 10 μM CD437, trypsinized, washed with phosphate-buffered saline (PBS), fixed with 3.7% paraformaldehyde, and stained with 50 μg of 4,6-diamidino-2-phenylindole (DAPI) per mL containing 100 μg of DNase-free RNase A per mL to visualize the nuclei. Stained cells are examined by fluorescence microscopy. For the terminal deoxynucleotidyl transferase (TdT) assay, cells are treated with or without 10 μM CD437. After treatment, cells are trypsinized, washed with PBS, fixed in 1% formaldehyde in PBS, washed with PBS, resuspended in 70% ice-cold ethanol, and immediately stored at -20°C overnight. Cells are then labeled with biotin-16-dUTP by terminal transferase and stained with avidin-FITC (fluorescein isothiocyanate).
激酶实验Forty microliter enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6 or 8 activity, 29 μL enzyme buffer and 1 μL resminostat [HCl] at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30 μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10 μM for HDAC6 and 25 μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 180 min (HDAC1, HDAC6, HDAC8) or 120 min (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/mL trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a Wallac Victor2 1420 multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the 50% inhibitory concentration (IC50) values the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) are set at 0% enzymatic activity (background fluorescence substracted).
动物实验Male Swiss-nu/nu mice weighing 20 to 25 g are used in this study. Mice are kept under sterile conditions at 24 to 26°C room temperature, 50% relative humidity, and 12 h light-dark rhythm in laminar flow shelves and are supplied with autoclaved food and bedding. For treatment of melanoma xenografts, previously established MeWo melanoma tumors of 1 to 2 mm in diameter are implanted into the right flank of animals. After tumor growth for 10 d, groups of mice (n=8) are either treated with saline p.o. or are injected intratumorally for 3 wk or are fed with various concentrations of CD437 (10 mg/kg/body weight and 30 mg/kg/body weight). In addition, tumors of a fifth group are injected with CD437 (10 mg/kg/body weight) each day. Mice are visited daily and growing tumors are measured twice weekly with a caliperlike instrument.
体外活性CD437 (10 µM,2天) 抑制这些肺癌细胞系的生长。剂量-反应实验显示,CD437减少了H460/SK-MES-1/A549/H292细胞数量(IC50:0.5/0.4/3/0.85 µM)。用CD437处理72小时,对所有黑色素瘤细胞系均表现出强烈的剂量依赖性生长抑制。在5 µM CD437浓度下,仅约5至25%的细胞在3天后保持存活。CD437所需的IC50浓度范围从对MeWo的10 µM到对SK-Mel-23的0.1 µM,显示出最高的敏感性。
体内活性在CD437处理的小鼠中,肿瘤停止生长,该效果在首次给药后的第3天和第13天已达到统计学意义(P<0.01),并在停药后3周以上仍然维持。组织学分析显示,CD437处理的肿瘤中,肿瘤-基质边缘处的c-fos mRNA水平显著增高。
存储条件store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 60 mg/mL (150.57 mM)
关键字inhibit | Retinoid X receptors | CD437 | RAR/RXR | Inhibitor | Autophagy | Retinoic acid receptors | CD-437 | CD 437
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AHPN|||O-Desmethyl Adapalene|||6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸|||Apoptosis Activator VI|TargetMol

公司简介

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。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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