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CD437

CD437

产品编号 T4371   CAS 125316-60-1
别名: AHPN, O-Desmethyl Adapalene, 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸, Apoptosis Activator VI

CD437 (AHPN) 是一种特异性视黄酸受体激动剂。

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CD437 Chemical Structure
CD437, CAS 125316-60-1
规格 价格/CNY 货期 数量
1 mg ¥ 262 现货
2 mg ¥ 369 现货
5 mg ¥ 578 现货
10 mg ¥ 912 现货
25 mg ¥ 1,890 现货
50 mg ¥ 3,150 现货
100 mg ¥ 4,590 现货
1 mL * 10 mM (in DMSO) ¥ 637 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
MG-132限时半价
重组蛋白限时优惠
产品目录号及名称: CD437 (T4371)
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纯度: 99.63%
纯度: 98.92%
纯度: 98.79%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.
体外活性 CD437 (10 μM, 2 days) inhibits the growth of these lung cancer cell lines. Dose-response experiments demonstrate that CD437 reduces the numbers of H460/SK-MES-1/A549/H292 cells (IC50: 0.5/0.4/3/0.85 μM). Treatment for 72 h with CD437 causes a strong dose-dependent growth inhibition in all melanoma cell lines. At a concentration of 5 μM CD437, only about 5 to 25% of the cells remain viable after 3 d. The concentrations of CD437 required for IC50 range from 10 μM for MeWo to 0.1 μM for SK-Mel-23 showing the highest sensitivity.
体内活性 Tumors in CD437-treated mice stop growing, an effect that becomes already statistically significant (P<0.01) at day 3 and 13 after first administration of CD437, and is maintained for more than 3 wk after discontinuation of treatment. Histologic analysis demonstrates marked c-fos mRNA levels at the tumor-stroma edge in CD437-treated tumors.
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).
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).
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.
别名 AHPN, O-Desmethyl Adapalene, 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸, Apoptosis Activator VI
分子量 398.49
分子式 C27H26O3
CAS No. 125316-60-1

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 150 mg/mL

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TargetMol Library Books参考文献

1. Li Y, et al. Molecular determinants of AHPN (CD437)-induced growth arrest and apoptosis in human lung cancer cell lines. Mol Cell Biol. 1998 Aug;18(8):4719-31. 2. Schadendorf D, et al. Treatment of melanoma cells with the synthetic retinoid CD437 induces apoptosis via activation of AP-1 in vitro, and causes growth inhibition in xenografts in vivo. J Cell Biol. 1996 Dec;135(6 Pt 2):1889-98.
Cecropin B acetate BMS 195614 K-8012 BMS493 Adapalene Ch55 LE135 Fluorobexarotene

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗代谢疾病化合物库 临床前化合物库 经典已知活性库 代谢化合物库 自噬库 脂代谢化合物库 细胞重编程化合物库 已知活性化合物库 表型筛选靶点鉴定库

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Keywords

CD437 125316-60-1 Autophagy Metabolism Retinoid Receptor inhibit Retinoid X receptors AHPN O-Desmethyl Adapalene RAR/RXR Inhibitor 6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸 Retinoic acid receptors Apoptosis Activator VI CD-437 CD 437 inhibitor

 

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