Home JAK/STAT STAT inhibitor HJC0152 For research use only.

HJC0152

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

HJC0152 Chemical Structure

HJC0152 Chemical Structure

CAS No. 1420290-99-8

Purity & Quality Control

Batch: S856101 DMSO]88 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.09%
99.09

HJC0152 Related Products

Signaling Pathway

STAT Signaling Pathways

STAT Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models MDA-MB-231 xenograft model (nude mice)
Dosages 2.5 and 7.5 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 406.65 Formula

C15H13Cl2N3O4.HCl
CAS No. 1420290-99-8 SDF Download HJC0152 SDF
Smiles C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)OCCN.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (216.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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