HPI-4 (Ciliobrevin A)

For research use only.

Catalog No.S8249 Synonyms: Hedgehog Pathway Inhibitor 4

3 publications

HPI-4 (Ciliobrevin A) Chemical Structure

CAS No. 302803-72-1

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.

Selleck's HPI-4 (Ciliobrevin A) has been cited by 3 publications

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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

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.

Assay
Methods Test Index PMID
Western blot
β-catenin; 

PubMed: 26515592     


Beta-catenin protein expression after 24 a. and 48 h b. after treatment with 10, 50 and 100 μM PNU-74654.

26515592
Growth inhibition assay
Cell viability; 

PubMed: 26515592     


NCI-H295 cell viability 24 a. 48 b. 72 c. and 96 d. hours after treatment with 5, 10, 50, 100 and 200 μM PNU-74654. HeLa cell viability 96 e. hours after treatment with 5, 10, 50, 100 and 200 μM PNU-74654. Y1 cell viability 48 h f. after treatment with 5, 10, 50, 100 and 200 μM PNU-74654. Cell viability was calculated by relative absorbance normalized by vehicle (DMSO). Values are reported as mean ± SEM. Statistics: ANOVA (a) *p = 0.0012; **p < 0.0001 (b) *p = 0.02; **p < 0.0001; (c) *p < 0.0001; **p = 0.03 (d) *p = 0.001, **p < 0.0001; (e) p = 0.05; (f) *p = 0.04.

26515592
In vivo Pancreatic fibrosis and destruction were effectively prevented by the treatment of HPI-4, a ciliogenesis inhibitor, in zebrafish model[3].

Protocol

Cell Research:[2]
- Collapse
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (198.22 mM)
Water Insoluble
Ethanol '1 mg/mL

* 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.

Chemical Information

Molecular Weight 358.18
Formula

C17H9Cl2N3O2

CAS No. 302803-72-1
Storage powder
in solvent
Synonyms Hedgehog Pathway Inhibitor 4
Smiles C1=CC=C2C(=C1)C(=O)NC(=N2)C(=C(C3=C(C=C(C=C3)Cl)Cl)O)C#N

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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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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID