Cyclopamine (Synonyms: 环巴胺; 11-Deoxojervine)

目录号: HY-17024 纯度: 99.95%: Data Sheet SDS COA 产品使用指南
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技术支持

Cyclopamine 是 Hedgehog 通路的拮抗剂，在细胞实验中的 IC₅₀ 为 46 nM。Cyclopamine 还是一种选择性的 Smo 抑制剂。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Cyclopamine Chemical Structure

CAS No. : 4449-51-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥543	In-stock
1 mg	￥272	In-stock
5 mg	￥600	In-stock
10 mg	￥900	In-stock
25 mg	￥1725	In-stock
50 mg	￥2700	In-stock
100 mg	￥4300	In-stock
200 mg	现货	询价
500 mg	现货	询价
1 g	现货	询价
5 g		询价
10 g		询价

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Customer Review

Other Forms of Cyclopamine:

Cyclopamine (Standard) 询价

MCE 顾客使用本产品发表的 47 篇科研文献

: Cyclopamine purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681. [Abstract]; Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 10 μM Cyc for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.

: Cyclopamine purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Sep 12;10(9):681. [Abstract]; Endometrial stromal cells are stimulated with 10 ng/mL TGFβ1 for 48 h. Then these cells are treated with 10 μM Cyc for 24 h and/or cocultured with 10 ng/mL VEGF165 for another 12 or 24 h. The protein levels of collagen 1, α-SMA and smad7 are examined.

: Cyclopamine purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 26:9:674. [Abstract]; Cyclopamine and GANT61 decrease the level of Gli1 as evidenced by western blot.

: Cyclopamine purchased from MCE. Usage Cited in: Int J Nanomedicine. 2017 Apr 20:12:3267-3280. [Abstract]; The Smo inhibitor Cyclopamine suppresses the activity of Hedgehog–Gli1 signaling. The gene expression and protein production of Smo in MG63 osteoblasts after 7 days of incubation on the different titanium surfaces.

: Cyclopamine purchased from MCE. Usage Cited in: Life Sci. 2017 Dec 15:191:82-89. [Abstract]; ORS cells are exposed to 3% oxygen for 48 h in presence or absence of Shh pathway inhibitor cyclopamine (5 μM) or GANT61 (10 μM). Immunofluorescence assay using anti-PCNA antibody is performed to detect the proliferative ORS cells (red). Cell nuclei are counterstained with DAPI (blue).

: Cyclopamine purchased from MCE. Usage Cited in: Neurochem Res. 2016 Apr;41(4):687-95. [Abstract]; Western blot and RT-qPCR assays of BDNF protein and gene expressions in primary cortical neurons in different experimental conditions. Immunoblotting bands of BDNF protein.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

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.

IC₅₀ & Target

Human Endogenous Metabolite

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	49 μM Compound: 1	Anticancer activity against human A549 cells by MTS assay Anticancer activity against human A549 cells by MTS assay	[PMID: 18221872]
C3H 10T1/2	EC₅₀	0.17 μM Compound: 1	Inhibition of Hedgehog pathway-dependent oxysterol-induced mouse C3 H10T1/2 cell differentiation assessed as alkaline phosphatase production after 72 hrs Inhibition of Hedgehog pathway-dependent oxysterol-induced mouse C3 H10T1/2 cell differentiation assessed as alkaline phosphatase production after 72 hrs	[PMID: 18842035]
C3H 10T1/2	IC₅₀	0.6 μM Compound: cyclopamine	Inhibition of human Shh-induced mouse C3H10T1/2 cell differentiation after 48 hrs by alkaline phosphatase reporter assay Inhibition of human Shh-induced mouse C3H10T1/2 cell differentiation after 48 hrs by alkaline phosphatase reporter assay	[PMID: 23074541]
C3H 10T1/2	IC₅₀	0.6 μM Compound: Cyclopamine	Inhibition of N-terminal SHH activated pathway in mouse C3H10T1/2 cells assessed as SAG-induced cell differentiation by alkaline phosphatase assay Inhibition of N-terminal SHH activated pathway in mouse C3H10T1/2 cells assessed as SAG-induced cell differentiation by alkaline phosphatase assay	[PMID: 21592788]
C3H 10T1/2	IC₅₀	0.62 μM Compound: Cyclopamine	Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs	[PMID: 22268551]
CHO	IC₅₀	1200 nM Compound: cyclopamine	Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay Antagonist activity at mouse Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay	[PMID: 19091559]
CHO	IC₅₀	280 nM Compound: cyclopamine	Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay Antagonist activity at human Smo receptor expressed in CHO cells by [3H]Hh-Ag binding assay	[PMID: 19091559]
Daoy	IC₅₀	0.16 μM Compound: 2, Cyc	Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis Inhibition of Hedgehog signaling in human DaOY cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by RT-PCR analysis	[PMID: 24900716]
HEK293	IC₅₀	64 nM Compound: Cyclopamine	Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy	[PMID: 22268551]
Medulloblastoma cell	EC₅₀	1 μM Compound: 16	Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay	[PMID: 17417631]
MEF	IC₅₀	1.9 μM Compound: cyclopamine	Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli-responsive betagalactosidase activity after 30 hrs by BetaGLo assay Inhibition of Smo in mouse Ptch-deficient MEF cells assessed as inhibition of Shh-induced Gli-responsive betagalactosidase activity after 30 hrs by BetaGLo assay	[PMID: 23074541]
Shh Light II	IC₅₀	0.3 μM Compound: Cyclopamine	Inhibition of SHH pathway in mouse Shh Light2 cells after 40 hrs by Gli-dependent luciferase reporter gene assay Inhibition of SHH pathway in mouse Shh Light2 cells after 40 hrs by Gli-dependent luciferase reporter gene assay	[PMID: 21592788]
Shh Light II	IC₅₀	0.3 μM Compound: Cyclopamine	Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay	[PMID: 22268551]
Shh Light II	IC₅₀	1312 nM Compound: Cyclopamine	Inhibition of SHH in mouse Shh-Light2 cells after 48 hrs by Gli1 reporter gene assay in presence of SAG Inhibition of SHH in mouse Shh-Light2 cells after 48 hrs by Gli1 reporter gene assay in presence of SAG	[PMID: 19541490]
Shh Light II	IC₅₀	484 nM Compound: Cyc	Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method Antagonist activity at Smo in mouse Shh-Light 2 cells assessed as inhibition of Shh-induced Gli1-reporter activity after 2 days by dual-luciferase reporter gene method	[PMID: 23063522]
Shh Light II	EC₅₀	500 nM Compound: 3	Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay	[PMID: 19309080]
TM3	IC₅₀	46 nM Compound: cyclopamine	Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay Inhibition of Hedgehog signaling pathway in mouse TM3 cells bearing pTA-8xGli-Luc reporter construct assessed as transcriptional modulation of Gli after 48 hrs by luciferase assay	[PMID: 19091559]
U-87MG ATCC	IC₅₀	22.5 μM Compound: Cyc	Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay Antiproliferative activity against human U87MG cells after 72 hrs by MTS assay	[PMID: 22226657]

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

411.62

Formula

C₂₇H₄₁NO₂

CAS 号

4449-51-8

性状

固体

颜色

White to off-white

中文名称

环杷明；环巴胺；11-去氧芥芬胺

结构分类

Steroids

初始来源

内源性代谢物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 5 mg/mL (12.15 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 5 mg/mL (12.15 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4294 mL	12.1471 mL	24.2943 mL
5 mM	0.4859 mL	2.4294 mL	4.8589 mL
10 mM	0.2429 mL	1.2147 mL	2.4294 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (1.21 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.5 mg/mL (1.21 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 0.5 mg/mL (1.21 mM); 澄清溶液

此方案可获得 ≥ 0.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.95%

选择批次：

Data Sheet (626 KB) SDS (393 KB)

COA (286 KB) HNMR (221 KB) LCMS (138 KB) 元素分析报告 (208 KB)

产品使用指南 (1538 KB)

参考文献

[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. [Content Brief]

[2]. Berman DM, et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature, 2003, 425(6960), 846-851. [Content Brief]

[3]. Thayer SP, et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature, 2003, 425(6960), 851-856. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Cell Assay ^[2]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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. [Content Brief] [2]. Berman DM, et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature, 2003, 425(6960), 846-851. [Content Brief] [3]. Thayer SP, et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature, 2003, 425(6960), 851-856. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Cyclopamine 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	2.4294 mL	12.1471 mL	24.2943 mL	60.7356 mL
	5 mM	0.4859 mL	2.4294 mL	4.8589 mL	12.1471 mL
	10 mM	0.2429 mL	1.2147 mL	2.4294 mL	6.0736 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cyclopamine4449-51-811-Deoxojervine环杷明环巴胺11-去氧芥芬胺HedgehogSmoEndogenous MetaboliteSmoothenedInhibitorinhibitorinhibit

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Cyclopamine (Synonyms: 环巴胺; 11-Deoxojervine)

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Other Forms of Cyclopamine:

MCE 顾客使用本产品发表的 47 篇科研文献

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Cyclopamine (Synonyms: 环巴胺; 11-Deoxojervine)

Customer Review

Other Forms of Cyclopamine:

Cyclopamine 相关抗体

MCE 顾客使用本产品发表的 47 篇科研文献

Cyclopamine 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

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参考文献

Cyclopamine 相关抗体:

摩尔计算器

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