Free shipping on all orders over $ 500

Cyclopamine

Cat. No. M1975
Cyclopamine Structure
Synonym:

11-deoxojervine

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 80  USD80 In stock
25mg USD 150  USD150 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM. Cyclopamine blocks the oncogenic effects of mutations of Ptch in fibroblasts and inhibits the growth of cells lacking Ptch function. Cyclopamine induced apoptosis in several small-cell lung cancer cell lines at 5 µM. Cyclopamine also be used to induce differentiation of human embryonic stem cells (hESCs) into hormone-expressing endocrine cells. Cyclopamine (11-deoxojervine) depletes stem-like cancer cells in glioblastoma and blocks tumor engraftment. Cyclopamine treatment significantly decreases of Snail mRNA and increasea E-cadherin transcripts in the E3LZ10.7 cell line in vitro. Administration of Cyclopamine alone profoundly inhibits tumor metastases in xenografts of E3LZ10.7 and L3.6pl, and completely abrogates metastases when in combination of gemcitabine.

Chemical Information
Molecular Weight 411.62
Formula C27H41NO2
CAS Number 4449-51-8
Solubility (25°C) Ethanol 5 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zhang J, et al. Bioorg Med Chem Lett. Synthesis and anticancer activity studies of cyclopamine derivatives.

[2] Bar EE, et al. Stem Cells. Cyclopamine-mediated hedgehog pathway inhibition depletes stem-like cancer cells in glioblastoma.

[3] Taipale J, et al. Nature. Effects of oncogenic mutations in Smoothened and Patched can be reversed by cyclopamine.

Related Hedgehog Products
TPB15

TPB15 is an orally potent Hh (Hedgehog) signaling inhibitor that significantly induces MDA-MB-468 cell cycle arrest and apoptosis. TPB15 also blocks Smo (Smoothened) translocation into cilia and reduces Smo protein and mRNA expression. In addition, TPB15 can inhibit the expression of downstream regulator Glioma-associated oncogene 1 (Gli1). TPB15 has good anti-tumor activity and low toxicity.

Hedgehog IN-3

Hedgehog IN-3 is a hedgehog pathway inhibitor (IC50 = 0.01 µM).

Hedgehog IN-5

Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway.

Hedgehog IN-2

Hedgehog IN-2 is an inhibitor of Hedgehog pathway with an IC50 value less than 0.003 μM in C3H10T1/2 cells.

Physalin H

Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC50 value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC50 values of 5.7 and 6.8 μM, respectively.

  Catalog
Abmole Inhibitor Catalog




Keywords: Cyclopamine, 11-deoxojervine supplier, Hedgehog, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.