Cyclopamine [Hedgehog (Hh) Inhibitor]
[CAT#: MOD2005ZP77]
Smo and hedgehog (Hh) signaling inhibitor. Also depletes stem like cancer cells.
- Target:
- Hedgehog
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Lot Number
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Lot Number
Description
Smo inhibitor and hedgehog (Hh) signal inhibitor. Prevent abnormal cell growth associated with fibroblast Ptch and Smo carcinogenic mutations. It also induces apoptosis and prevents the cell cycle in the G0/G1 phase, and depletes stem cells like cancer cells. Show anticancer activity.
Chemical Name
(2'R,3S,3'R,3'aS,6'S,6aS,6bS,7'aR,11aS,11bR)-1,2,3,3'a,4,4',5',6,6',6a,6b,7,7',7'a,8,11,11a,11b-Octadecahydro-3',6',10,11b-tetramethylspiro[9H-benzo[a]fluorene-9,2'(3'H)-furo[3,2-b]pyridin]-3-ol
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
Using small molecule Hh inhibitors such as HhAntag and the natural product Cyclopamine combined with Smo can induce tumor remission in a genetic mouse model of medulloblastoma [1]. Cyclopamine is a Hedgehog (Hh) pathway antagonist. Cyclopamine inhibits cell growth. Cyclopamine (3μM) inhibits Hh pathway activity and the growth of gastrointestinal tumor cell lines is related to PTCHmRNA expression [2]. Cyclopamine is a steroid alkaloid that can inhibit Hh signaling through direct interaction with Smo [3].
Reference
[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.
[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.
Assay Description
Cyclopamine can lead to persistent regression of xenograft tumors. Tumors in animals treated with cyclopamine completely resolved after 12 days [1]. Cyclopamine (1.2 mg) treatment can block the formation of transplanted tumors of human pancreatic cancer in nude mice [2].
References
[1]. Berman DM, et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature, 2003, 425(6960), 846-851.
[2]. Thayer SP, et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature, 2003, 425(6960), 851-856.
[2]. Thayer SP, et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature, 2003, 425(6960), 851-856.
Molecular Weight
411.62
Form
Powder
Chemical Formula
C27H41NO2
Source
Synthetic
SMILES
O[C@H](C2)CC[C@@]1(C)C2=CC[C@]([C@@]([H])3CC[C@@]54O[C@@](C[C@H](C)CN6)([H])[C@]6([H])[C@H]5C)([H])[C@@]([H])1CC3=[C@@]4C
CAS NO.
4449-51-8
PubChem Substance ID
442972
Purity
>98%
Storage
Store at +4°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -31°C for several months.
Research Use Only
For research use only
For Research Use Only. Not For Clinical Use.
