[CAS NO. 302803-72-1]  HPI-4 (Ciliobrevin A)

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PRODUCTS SPECIFICATIONS [302803-72-1]

Catalog
SLK-S8249
Brand
Selleck
CAS
302803-72-1

DESCRIPTION [302803-72-1]

Overview

MDLMFCD01911757
Molecular Weight358.18
Molecular FormulaC17H9Cl2N3O2
SMILESN#C/C(C(C1=CC=C(Cl)C=C1Cl)=O)=C(N2)/NC3=C(C=CC=C3)C2=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.7919 mL13.9595 mL27.9189 mL
5 mM0.5584 mL2.7919 mL5.5838 mL
10 mM0.2792 mL1.3959 mL2.7919 mL
50 mM0.0558 mL0.2792 mL0.5584 mL

Description

HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a 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. 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). HPI-4(ciliobrevin A) is also a small molecule inhibitor of the catalytic heavy chain subunit of cytoplasmic dynein.

In vivo

Pancreatic fibrosis and destruction were effectively prevented by the treatment of HPI-4, a ciliogenesis inhibitor, in zebrafish model.