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- CAS号：
4449-51-8
- 规格：
1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥359.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥387.0 |
| 规格： | 10mg | 产品价格： | ￥602.0 |
| 规格： | 25mg | 产品价格： | ￥1104.0 |
| 规格： | 50mg | 产品价格： | ￥1810.0 |
| 规格： | 100mg | 产品价格： | ￥2878.0 |
Product Introduction
Bioactivity
| 名称 | Cyclopamine |
| 描述 | Cyclopamine (11-Deoxojervine) is a natural small molecule steroidal alkaloid extracted from plants of the genus Aconitum. Cyclopamine acts as an antagonist of the Hedgehog pathway with an IC50 of 46 nM in cellular assays. Additionally, Cyclopamine functions as a selective Smo inhibitor. Cyclopamine is applicable for research in embryonic development, tumorigenesis, and targeted therapies. |
| 细胞实验 | Cells were cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody, ShhNp and/or cyclopamine were added at 0 h at concentrations indicated in the main text. Viable cell mass was determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth was calculated as OD (day 4) 2 OD (day 2)/OD (day 2) [3]. |
| 激酶实验 | This assay measures the end stage of the Hh signaling pathway, that is, the transcriptional modulation of Gli, using Luciferase as readout (Gli-Luc assay). Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are resuspended in F12 Ham's/DMEM (1:1) containing 5% FBS and 15 mM Hepes pH 7.3, added to assay plates and incubated with Cyclopamine for approximately 30 minutes at 37 °C in 5% CO2. 1 nM Hh-Ag 1.5 is then added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 value, defined as the inflection point of the logistic curve, is determined by non-linear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of Cyclopamine using the R statistical software pack [1]. |
| 动物实验 | A total of 0.1 ml Hanks' balanced salt solution and matrigel (1:1) containing 2 × 10^6 cells were injected subcutaneously into CD-1 nude mice. Tumours were grown for 4 days to a minimum volume of 125 mm3; treatment was initiated simultaneously for all subjects. Mice were injected subcutaneously with vector alone (triolein:ethanol 4:1 v/v) or a cyclopamine suspension (1.2 mg per mouse in triolein: ethanol 4:1 v/v) daily for 7 days. At the end of the treatment period, tumours were excised from mice, weighed and then fixed for 3 h at 4 °C with 4% paraformaldehyde, embedded in paraffin wax and sectioned (6 μm). Apoptotic cells were identified by TUNEL using recombinant Tdt as previously described29. Sections were then counterstained with eosin. Eight ×20-magnified fields from regions corresponding to the exterior, middle and interior of two control and two cyclopamine-treated tumours were chosen at random [5]. |
| 体外活性 | 方法：从 C57BL/6N 小鼠分离的原代肝细胞，加入 Cyclopamine （10 μM）和雷帕霉素 （50 nM），处理 24 小时，Seahorse XF 分析仪检测线粒体耗氧率（OCR），计算基础呼吸、最大呼吸、ATP 产量等参数。 结果：Cyclopamine 与雷帕霉素联合显著降低最大呼吸和 ATP 产量。[1] 方法：HeLa 细胞中加入 Cyclopamine （5 μM），处理 24 小时，Western blot 检测 cathepsin D 的成熟形式（31 kDa）与未成熟形式（53 kDa）的比值。 结果：Cyclopamine 处理导致成熟/未成熟 cathepsin D 比值显著降低，表明溶酶体成熟受损。[2] |
| 体内活性 | 方法：转基因果蝇，在眼部表达 APP-C99-Gal4 和 UAS-GRIM(γ-分泌酶切割后激活 GRIM，导致眼粗糙)，果蝇从幼虫至成体在含 Cyclopamine 药(100 nM)食物上饲养，成体后 24 小时内观察。 结果：Cyclopamine 处理组果蝇的粗糙眼表型严重程度显著降低，在体内也能减少γ-分泌酶介导的 APP 切割。[2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 4.12 mg/mL (10.01 mM), Sonication is recommended. |
| 关键字 | Smoothened | Smo | Inhibitor | inhibit | Hedgehog | EndogenousMetabolite | Endogenous Metabolite | Cyclopamine |
| 相关产品 | Guanidine hydrochloride | Glycerol | Aceglutamide | Malic acid | DL-Lysine | Sucrose | Guanidine thiocyanate | Nicotinamide riboside malate | Gluconate Calcium | Thymidine | Corn starch | D(+)-Raffinose pentahydrate |
| 相关库 | Bioactive Compound Library | Bioactive Compounds Library Max | Selected Plant-Sourced Compound Library | Ancient Chinese Classical Formulas Compound Library | Alkaloid Natural Product Library | Miao medicine Compound Library | Food as Medicine Compound Library | Anti-Tumor Natural Product Library | Traditional Chinese Medicine Monomer Library | Natural Product Library | GPCR Compound Library | Membrane Protein-targeted Compound Library |
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