Jervine

Synonyms: 11-Ketocyclopamine

Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.

Jervine Chemical Structure

Jervine Chemical Structure

CAS No. 469-59-0

Purity & Quality Control

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
s12 cells Function assay Inhibition of lipid-modified (octylated) form of SHH expressed in mouse s12 cells by luciferase reporter gene assay, IC50=0.5 μM 19309080
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Biological Activity

Description Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.
Targets
Hedgehog [1] Shh [1]
In vitro
In vitro Compared to controls, chondrocyte cultures exposed to 25 μg/ml jervine shows an apparent reduction in cell number but no differences in cellular morphology or relative intensity of alcian blue staining[2].
Cell Research Cell lines C3H/10T 1/2 CL8 cells
Concentrations 5, 10, or 25 μg/ml
Incubation Time 48 h
Method

Cells are grown in Eagle's basal medium supplemented with 10% fetal bovine serum and 0.25 mg/ml gentamicin sulfate. Cells are seeded onto 35-mm tissue culture plates at a density of 1×104 celldplate. The plated cells are incubated for 24 hours prior to treatment in a humidified incubator at 37 "C in an atmosphere of 5% CO2 in air. Drugs are then added: jervine to a final concentration of 5, 10, or 25 μg/ml; retinoic acid at 0.03, 0.30, or 3.0 pg/ml. After a final 48 hours of incubation, media are removed, the cultures are rinsed three times with phosphate-buffered saline (PBS) pH 7.4, and the cells are harvested into 0.5 ml of 0.1% (w/v) trypsin which contained 0.1% EDTA (w/v) in PBS. Each sample is mixed with 9.5 ml Isoton Ⅱ, and cell numbers are determined by using a Coulter Counter.

In Vivo
In vivo Embryos exposed to jervine develop craniofacial abnormalities related to those found in Shh mutant embryos. The lower jaw of these embryos is severely reduced in size, often leading to loss of the incisors. Treatment of pregnant mice with the hedgehog inhibitor jervine induces jaw defects in the embryos similar to those found in Prx1−/−Prx2−/− embryos. The distal part of the jaw is reduced in size, and both incisors are absent[1].
Animal Research Animal Models A/J mice
Dosages 400 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 425.60 Formula

C27H39NO3

CAS No. 469-59-0 SDF Download Jervine SDF
Smiles CC1CC2C(C(C3(O2)CCC4C5CC=C6CC(CCC6(C5C(=O)C4=C3C)C)O)C)NC1
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 10 mg/mL ( (23.49 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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