| CAS |
No.4449-51-8 |
| 中文名称 |
环巴胺(10mM in DMSO,无菌） |
| 英文名称 |
Cyclopamine(10mM in DMSO，Sterile） |
| 分子式 |
C27H41NO2 |
| 分子量 |
411.62 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Hedgehog，Smoothened |
| 通路 |
Hedgehog;Stem Cells |
| 背景说明 |
Cyclopamine是一种特异性Hedgehog信号通路拮抗剂。 |
| 生物活性 |
Cyclopamine is a Hedgehog (Hh) pathway antagonist with an IC50 of 46 nM in the Hh cell assay. Cyclopamine is also a selective Smo inhibitor.[1-5] |
| In Vitro |
Treatment with small molecule Hh inhibitors such as HhAntag and the natural product Cyclopamine， both binding to Smo， induces tumor remission in a genetic mouse model of medulloblastoma[1]. Cyclopamine is a Hedgehog (Hh) pathway antagonist. Cyclopamine suppresses cell growth. Cyclopamine (3 μM) suppression of Hh pathway activity and growth in digestive tract tumour cell lines correlates with expression of PTCHmRNA[2]. Cyclopamine is a steroidal alkaloid that inhibits Hh signalling through direct interaction with Smo[3]. |
| In Vivo |
Cyclopamine causes durable regression of xenograft tumors. Tumors in Cyclopamine-treated animals， regress completely by 12 days[2]. Cyclopamine (1.2 mg) treatment blocks tumour formation of human pancreatic adenocarcinoma cells after transplantation into nude mice[3]. |
| 细胞实验 |
Cells are cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody， ShhNp and/or Cyclopamine (3 μM) are added at 0 h at concentrations indicated in the main text. Viable cell mass is determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth is calculated as OD (day 4)-OD (day 2)/OD (day 2)[2]. |
| 动物实验 |
Mice[3]A total of 0.1 mL Hanks’ balanced salt solution and matrigel (1:1) containing 2×106 cells is injected subcutaneously into CD-1 nude mice. Tumors are grown for 4 days to a minimum volume of 125 mm3; treatment is initiated simultaneously for all subjects. Mice are 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 are 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 are identified by TUNEL using recombinant Tdt. Sections are 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 are chosen at random. We counted the number of TUNEL-positive nuclei manually. Haematoxylin/eosin staining is done. |
| 数据来源文献 |
[1]. Peukert S， et al. Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorg Med Chem Lett， 2009， 19(2)， 328-331.
[2]. Berman DM， et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature， 2003， 425(6960)， 846-851.
[3]. Thayer SP， et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature， 2003， 425(6960)， 851-856.
[4]. Ma W， et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer‘s disease. J Genet Genomics. 2018 May 20;45(5):237-246.
[5]. Qi Wan， et al. Overexpression of Laminin α4 Facilitates Proliferation and Migration of Fibroblasts in Knee Arthrofibrosis by Targeting Canonical Shh/Gli1 Signaling. Connect Tissue Res. 2020 May 24. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
说明书下载
京公网安备 11011202000391号