Cyclopamine 是Hedgehog通路的拮抗劑，細(xì)胞實(shí)驗(yàn)中IC50=46 nM。它還是選擇性Smo抑制劑。

環(huán)巴胺的EC50是10.57微米，這是通過FXR-bla(法尼基X受體-β-內(nèi)酰胺酶)分析確定的[3]。 Hh信號通路在胚胎發(fā)育和腫瘤發(fā)生中起著關(guān)鍵作用[4]。Hh信號通路在廣泛的人類組織中顯示出調(diào)節(jié)細(xì)胞增殖和分化的顯著性。它與許多人類惡性腫瘤中的異常細(xì)胞存活有關(guān)，從基底細(xì)胞癌和髓母細(xì)胞瘤到小細(xì)胞肺、胃腸道、乳腺和前列腺腫瘤[1]。

暴露于環(huán)巴胺的胚胎導(dǎo)致可見的外部缺陷，包括獨(dú)眼畸形、長鼻形成、小眼癥、胸部前凸、阿米莉亞和體型減小。對胃腸器官的檢查顯示了嚴(yán)重的缺陷，包括腸管長度縮短和前腸衍生器官中的間充質(zhì)細(xì)胞數(shù)量減少。在十二指腸、胃和背胰腺中也發(fā)現(xiàn)了異位結(jié)構(gòu)[5]。

產(chǎn)品性質(zhì)：

Cas No.：4449-51-8

別名：環(huán)巴胺; 11-Deoxojervine

化學(xué)名： (3S,3'R,3'aS,6'S,6aS,6bS,7'aR,9R,11aS,11bR)-3',6',10,11b-tetramethylspiro[2,3,4,6,6a,6b,7,8,11,11a-decahydro-1H-benzo[a]fluorene-9,2'-3a,4,5,6,7,7a-hexahydro-3H-furo[3,2-b]pyridine]-3-ol

Canonical SMILES CC1CC2C(C(C3(O2)CCC4C5CC=C6CC(CCC6(C5CC4=C3C)C)O)C)NC1

分子式：C27H41NO2

分子量：411.62

溶解度：≥ 6.9mg/mL in DMSO

儲存條件：Store at -20°C

注意事項(xiàng)：

為了您的安全和健康，請穿實(shí)驗(yàn)服并戴一次性手套操作。

References:

[1].  Marc J. Meth and Jeffrey M. Weinberg. Cyclopamine: Inhibiting Hedgehog in the Treatment of Psoriasis. Continuing Medical Education, 2006, 78: 185-188.

[2].  Jun Che, Fu-Zheng Zhang, Chao-Qian Zhao, et al. Cyclopamine is a novel Hedgehog signaling inhibitor with significant anti?proliferative, anti?invasive and anti?estrogenic potency in human breast cancer cells. Oncology Letters, 2013, 5: 1417-1421.

[3].  Chia-Wen Hsu, Jinghua Zhao, Ruili Huang, et al. Quantitative High-Throughput Profiling of Environmental Chemicals and Drugs that Modulate Farnesoid X Receptor. Scientific Reports, 2014, 4: 6437.

[4].  Robert J. Lipinski, Paul R. Hutson, Paul W. Hannam, et al. Dose- and Route-Dependent Teratogenicity, Toxicity, and Pharmacokinetic Profiles of the Hedgehog Signaling Antagonist Cyclopamine in the Mouse. Toxicological Sciences, 2008, 104(1):189-197.

[5].  Seung K. Kim and Douglas A. Melton. Pancreas development is promoted by cyclopamine, a Hedgehog signaling inhibitor. Proc. Natl. Acad. Sci. USA, 1998, 95: 13036-13041.