HPI-4 (Ciliobrevin A)

Catalog No.S8249 Batch:S824901

Technical Data

Formula	C₁₇H₉Cl₂N₃O₂
Molecular Weight	358.18	CAS No.	302803-72-1
Solubility (25°C)*	In vitro	DMSO	71 mg/mL (198.22 mM)
		Ethanol	1 mg/mL (2.79 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.

In vivo

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

Protocol (from reference)

Cell Assay:^{^[2]}	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.

Cell Assay:^{^[2]}

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.

References

Selleck's HPI-4 (Ciliobrevin A) has been cited by 7 publications

RNA localization mechanisms transcend cell morphology [ Elife, 2023, 12e80040]	PubMed: 36867563
Primary Cilia Restrain PI3K-AKT Signaling to Orchestrate Human Decidualization [ Int J Mol Sci, 2022, 23(24)15573]	PubMed: 36555215
Primary Cilia Restrain PI3K-AKT Signaling to Orchestrate Human Decidualization [ Int J Mol Sci, 2022, 23(24)15573]	PubMed: 36555215
HeLa Cervical Cancer Cells Are Maintained by Nephronophthisis 3-Associated Primary Cilium Formation via ROS-Induced ERK and HIF-1α Activation under Serum-Deprived Normoxic Condition [ Int J Mol Sci, 2022, 23(23)14500]	PubMed: 36498831
Discoidin domain receptor 1 regulates endochondral ossification through terminal differentiation of chondrocytes. [ FASEB J, 2020, 10.1096/fj.201901852RR]	PubMed: 32128899
Evodiamine Augments NLRP3 Inflammasome Activation and Anti-bacterial Responses Through Inducing α-Tubulin Acetylation. [ Front Pharmacol, 2019, 10:290]	PubMed: 30971927
Crosstalks of the PTPIP51 interactome revealed in Her2 amplified breast cancer cells by the novel small molecule LDC3/Dynarrestin. [ PLoS One, 2019, 14(5):e0216642]	PubMed: 31075141

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