Jervine

Catalog No.S4747 Batch:S474701

Technical Data

Formula	C₂₇H₃₉NO₃
Molecular Weight	425.60	CAS No.	469-59-0
Solubility (25°C)*	In vitro	DMSO	5 mg/mL (11.74 mM)
		Ethanol	2 mg/mL (4.69 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

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].

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].

Protocol (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[1]}	Animal Models A/J mice Dosages 400 mg/kg Administration oral administration

Cell Assay:^{^[2]}

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.

Animal Study:^{^[1]}

Animal Models
A/J mice
Dosages
400 mg/kg
Administration
oral administration

References

Selleck's Jervine has been cited by 2 publications

Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7]	PubMed: 34997030
Down-regulation of astrocytic sonic hedgehog by activation of endothelin ETB receptors: Involvement in traumatic brain injury-induced disruption of blood brain barrier in a mouse model [ Neurochem Int, 2021, 146:105042]	PubMed: 33838160

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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