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HJC0152 STAT inhibitor

Name: HJC0152
Brand: Selleck Chemicals
SKU: S8561
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S8561

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

Chemical Structure

Molecular Weight: 406.65

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.09

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Chemical Information, Storage & Stability

Molecular Weight	406.65	Formula	C₁₅H₁₃Cl₂N₃O₄.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1420290-99-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=C(C=C1[N+](=O)[O-])Cl)NC(=O)C2=C(C=CC(=C2)Cl)OCCN.Cl

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.400mg/ml (10.82mM)	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (2.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound induces cleaved caspase-3 and downregulated cyclin D1 in MDA-MB-231 cells, inhibits cell cycle progression and promotes apoptosis^[1]. This chemical 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, it 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. This compound does not show significant signs of toxicity at a dose of 75 mg/kg^[1]. In SCC25-derived orthotopic mouse models, this chemical treatment significantly abrogates STAT3/β-catenin expression in vivo, which leading to a global decrease of tumor growth and invasion^[2].
References	https://pubmed.ncbi.nlm.nih.gov/23459613/ https://pubmed.ncbi.nlm.nih.gov/23459613/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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