HJC0152

For research use only.

Catalog No.S8561

2 publications

HJC0152 Chemical Structure

CAS No. 1420290-99-8

HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.

Selleck's HJC0152 has been cited by 2 publications

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Biological Activity

Description HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
Targets
STAT3 [1]
()
In vitro

HJC0152 inhibits STAT3 promoter activity in MDA-MB-231 cells in a dose-dependent manner. It has a comparable potency in downregulating STAT3 protein production and phosphorylation at the Tyr-705 site. HJC0152 induces cleaved caspase-3 and downregulated cyclin D1 in MDA-MB-231 cells, inhibits cell cycle progression and promotes apoptosis[1]. HJC0152 treatment efficiently suppresses HNSCC cell proliferation, arrests the cell cycle at the G0/G1 phase, induces apoptosis, and reduced cell invasion in both SCC25 and CAL27 cell lines. Moreover, HJC0152 inhibits nuclear translocation of phosphorylated STAT3 at Tyr705 and decreases VHL/β-catenin signaling activity via regulation of microRNA-21[2].

In vivo HJC0152 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo (ip and po), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancer. It has an improved oral bioavailability and an enhanced suppression of tumor growth in mice. HJC0152 does not show significant signs of toxicity at a dose of 75 mg/kg[1]. In SCC25-derived orthotopic mouse models, HJC0152 treatment significantly abrogates STAT3/β-catenin expression in vivo, which leading to a global decrease of tumor growth and invasion[2].

Protocol

Cell Research:

[1]

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  • Cell lines: MDA-MB-231 breast cancer cells
  • Concentrations: 1, 5, and 10 μM
  • Incubation Time: 24 h
  • Method:

    The cells are treated with different doses of compound 11 for 24 h, and levels of total STAT3 and phosphorylated STAT3 at Tyr-705 are then examined by Western blot.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: MDA-MB-231 xenograft model (nude mice)
  • Dosages: 2.5 and 7.5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (216.4 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 406.65
Formula

C15H13Cl2N3O4.HCl

CAS No. 1420290-99-8
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)OCCN.Cl

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID