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Purity: ≥98%
Ciliobrevin A, formerly known as HPI-4 and Hedgehog Pathway Inhibitor 4, is a Hedgehog pathway inhibitor. Treatment with HH pathway inhibitor-4 (HPI-4) could significantly decrease human chondrosarcoma cell proliferation, invasion and migration ability. Furthermore, HPI-4 could distinctly disturb HH pathway-mediated ciliogenesis and suppress primary cilia-related protein intraflagellar transport protein IFT88 expression. HH downstream effect molecular GLI2 was restrained to block parathyroid hormone-related protein and affect MAPK/ERK-regulated matrix metalloproteinases (MMP2 and MMP9). d HPI-4 could be a new therapeutic option specific to chondrosarcoma expressing elevated levels of HH pathway.
| ln Vitro |
While HPI-2 and HPI-3 exhibited no discernible effect, ciliobrevin A (HPI-4) likewise stopped the rise in the FLAG-Gli2 full-length/repressor protein ratio following Shh stimulation. While HPI-2 or HPI-3 had no discernible influence on FLAG-Gli1 levels, Ciliobrevin A decreased the stability of FLAG-Gli1 in these cells, exposing a different mechanism by which this small chemical inhibits Hh target gene production. The effect of ciliobrevin A on ciliary FLAG-Gli2 levels is greater than that of the compound on total FLAG-Gli2 levels. Additionally, primary cilia in Shh-EGFPFLAG-Gli2 cells cultivated with Ciliobrevin A were shortened, and in the majority of Ciliobrevin A-treated cells, this organelle was gone. Additionally, in Shh-LIGHT2FLAG-Gli1 cells, ciliobrevin A interferes with the development of primary cilia and encourages FLAG-Gli1 accumulation at the distal end of this organelle. As shown by histone H3 phosphorylation (pH3), cleiobrevin A markedly suppressed the proliferation of these neural progenitor cells. It also decreased the amounts of cyclin D1 protein, Gli1, Gli2, and N-Myc transcripts in CGNPs. While Cyclopamine, a Smo inhibitor, is ineffective against any oncogenic lesions, Ciliobrevin A effectively inhibits the proliferation of SmoM2-expressing CGNPs and is also effective against CGNPs lacking Su(fu) function [1].
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| References |
[1]. Hyman JM, et al. Small-molecule inhibitors reveal multiple strategies for Hedgehog pathway blockade. Proc Natl Acad Sci U S A. 2009 Aug 18;106(33):14132-7
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| Molecular Formula |
C17H9CL2N3O2
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|---|---|
| Molecular Weight |
358.178
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| Exact Mass |
357.0072
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| CAS # |
302803-72-1
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| Related CAS # |
302803-72-1;
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| SMILES |
N#C/C(C(C1=CC=C(Cl)C=C1Cl)=O)=C(N2)/NC3=C(C=CC=C3)C2=O
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| InChi Code |
InChI=1S/C17H9Cl2N3O2/c18-9-5-6-10(13(19)7-9)15(23)12(8-20)16-21-14-4-2-1-3-11(14)17(24)22-16/h1-7,21H,(H,22,24)/b16-12+
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| Chemical Name |
(E)-3-(2,4-dichlorophenyl)-3-oxo-2-(4-oxo-3,4-dihydroquinazolin-2(1H)-ylidene)propanenitrile
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| Synonyms |
Ciliobrevin A HPI-4 HPI 4 HPI4. Hedgehog Pathway Inhibitor 4.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~279.19 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7919 mL | 13.9595 mL | 27.9189 mL | |
| 5 mM | 0.5584 mL | 2.7919 mL | 5.5838 mL | |
| 10 mM | 0.2792 mL | 1.3959 mL | 2.7919 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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