Home Stem Cells & Wnt Hedgehog/Smoothened inhibitor HPI-4 (Ciliobrevin A) For research use only.

HPI-4 (Ciliobrevin A)

Synonyms: Hedgehog Pathway Inhibitor 4

HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

HPI-4 (Ciliobrevin A) Chemical Structure

HPI-4 (Ciliobrevin A) Chemical Structure

CAS: 302803-72-1

Selleck's HPI-4 (Ciliobrevin A) has been cited by 6 publications

Purity & Quality Control

Batch: S824901 DMSO] 71 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.63%
99.63

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Biological Activity

Description HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.
Targets
Hedgehog [1]
In vitro
In vitro HPI-4 does not directly target Smo. It counteracts the activities of endogenous Gli1 and Gli2 but does not directly act on transcription factor GLIs. HPI-4 significantly inhibited the proliferation of these neuronal progenitors, as measured by histone H3 phosphorylation (pH3) levels, It also reduced cellular levels of cyclin D1 protein and Gli1, Gli2, and N-Myc transcripts in the Cerebellar Granule Neuron Precursors. HPI-4 acts by perturbing ciliogenesis[1]. 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)[2]. HPI-4(ciliobrevin A) is also a small molecule inhibitor of the catalytic heavy chain subunit of cytoplasmic dynein.
Cell Research Cell lines The human chondrosarcoma cell line SW1353
Concentrations 0, 5 and 10 μM
Incubation Time 0, 1, 3, 6 and 9 days
Method 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot β-catenin 26515592
Growth inhibition assay Cell viability 26515592
In Vivo
In vivo Pancreatic fibrosis and destruction were effectively prevented by the treatment of HPI-4, a ciliogenesis inhibitor, in zebrafish model[3].

Chemical Information & Solubility

Molecular Weight 358.18 Formula

C17H9Cl2N3O2
CAS No. 302803-72-1 SDF Download HPI-4 (Ciliobrevin A) SDF
Smiles C1=CC=C2C(=C1)C(=O)NC(=N2)C(=C(C3=C(C=C(C=C3)Cl)Cl)O)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (198.22 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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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.

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