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Ciliobrevin A

Catalog No. T3156 CAS 302803-72-1

Synonyms: Hedgehog Pathway Inhibitor 4, HPI-4

Ciliobrevin A (HPI-4) is an inhibitor of hedgehog signaling pathway with an IC50 <10 μM.

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Ciliobrevin A, CAS 302803-72-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 57.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 177.00
50 mg	In stock	$ 317.00
100 mg	In stock	$ 547.00
200 mg	In stock	$ 698.00
500 mg	In stock	$ 1,090.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.22%

Purity: 97.10%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Ciliobrevin A (HPI-4) is an inhibitor of hedgehog signaling pathway with an IC50 <10 μM.
Targets&IC50	Hedgehog:>10 μM.
In vitro	Shh-EGFPFLAG-Gli2 cells cultured with Ciliobrevin A have truncated primary cilia, and this cellular organelle is absent in a significant fraction of Ciliobrevin A-treated cells. Ciliobrevin A perturbs primary cilia formation in the Shh-LIGHT2FLAG-Gli1 cells and promotes accumulation of FLAG-Gli1 at the distal tip of this organelle. Ciliobrevin A significantly inhibits the proliferation of these neuronal progenitors, as measured by histone H3 phosphorylation (pH3) levels, and reduces cellular levels of cyclin D1 protein and Gli1, Gli2, and N-Myc transcripts in the CGNPs. Ciliobrevin A can block the proliferation of SmoM2-expressing CGNPs and should be equally potent against CGNPs lacking Su(fu) function, whereas the Smo inhibitor Cyclopamine is ineffective against either oncogenic lesion. Ciliobrevin A prevents an increase in the FLAG-Gli2 full-length/repressor ratio upon Shh stimulation, but HPI-2 and HPI-3 have no significant effect. Ciliobrevin A increases ciliary levels of FLAG-Gli2 in a manner disproportionate to their effects on total FLAG-Gli2 levels[1].
Kinase Assay	Smo-binding assays are conducted with BODIPY-cyclopamine and Smo-overexpressing HEK 293T cells, using a CMVpromoter-based SV40 origin-containing expression construct for Smo-Myc3 (murine Smo containing three consecutive Myc epitopes at the C terminus). HEK 293T cells are seeded into eight-well chambered coverslips (80,000 cells/well) and cultured in DMEM containing 10% FBS, 100 U/mL penicillin, and 0.1 mg/mL streptomycin. The cells are cultured until they reached 55 to 65% confluency (14-18 h), after which they are transfected with the Smo-Myc3 expression construct and Transit-LT1. Twenty-four hours after transfection, the cells are washed with PBS and cultured in DMEM containing 0.5% FBS, 5 nM BODIPY-cyclopamine, and various concentrations of either cyclopamine or individual HPIs. After 30 min, 10 μM Hoescht 33342 is added to each well, and the HPIs are incubated with the cells for an additional 30 min. The cells are then washed two times with PBS buffer, once with phenol red-free DMEM containing 0.5% FBS, and immediately imaged using a DMI6000B compound microscope. Images are background-substracted using ImageJ software with a rolling ball size of 75 pixels, and BODIPY-cyclopamine intensity is then determined using Metamorph software. Circular regions with a diameter of 300 pixels are placed over regions containing uniformly confluent cells, and the pixel intensities of approximately 20 regions from four independent images is used to determine the average BODIPY-cyclopamine levels for each experimental condition[1].
Cell Research	Using MTS-8 assay to measure cell proliferation and the toxicity of this drug. 2000 cells were plated in 96-well plates per well. HPI-4 was added to cells at concentrations of 0, 5 and 10 μM in 100 μl DMEM/F12 with 10% FBS and incubated for 0, 1, 3, 6 and 9 days. Then, 10 μl MST-8 was added to the media in each well and incubated in an environment without light for 90 min. The absorbance value was measured using an enzyme microplate reader at 450 nm wavelength. The relative viability of cells was expressed by OD value.(Only for Reference)

Synonyms	Hedgehog Pathway Inhibitor 4, HPI-4
Molecular Weight	358.18
Formula	C17H9Cl2N3O2
CAS No.	302803-72-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 70 mg/mL (195.43 mM)

Ethanol: 1 mg/mL (2.79 mM)

References and Literature

1. Hyman JM, et al. Proc Natl Acad Sci U S A. 2009, 106(33):14132-7. 2. Xiang W, et al. Oncol Rep. 2014, 32(4):1622-30. 3. Jung IH, et al. PLoS One. 2011, 6(12):e27941.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Anti-Cancer Compound Library Reprogramming Compound Library NO PAINS Compound Library Anti-Prostate Cancer Compound Library Stem Cell Differentiation Compound Library Wnt/Hedgehog/Notch Compound Library Anti-Aging Compound Library Bioactive Compound Library

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Keywords

Ciliobrevin A 302803-72-1 GPCR/G Protein Stem Cells Hedgehog/Smoothened Hedgehog Pathway Inhibitor 4 Hedgehog HPI 4 HPI-4 HPI4 inhibit Inhibitor inhibitor

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