| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
STAT3
STAT3 (Signal Transducer and Activator of Transcription 3). STAT3-IN-15 is a STAT3 inhibitor that binds to the SH2 domain of STAT3, preventing its phosphorylation at Tyr705, which is essential for STAT3 dimerization, nuclear translocation, and transcriptional activation. STAT3 is a transcription factor involved in cell survival, proliferation, and fibrosis. |
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| ln Vitro |
Compound 10k, STAT3-IN-15, has an IC50 of 0.47 μM, which reduces the growth of NIH-3T3 cells [1]. STAT3-IN-15 resides in the pY subpocket of STAT3 and makes hydrogen bonds with Ser636 and Lys591. [1]. Inhibiting fibroblast activation and proliferation, STAT3-IN-15 (0-100 nM, 72 h) [1]. NIH-3T3 cells' activation mediated by TGF-β1 (5 ng/mL) is inhibited by STAT3-IN-15 (50 nM, 24 h) [1]. In A549 cells, TGF-β1-induced EMT (morphological alterations) is blocked by STAT3-IN-15 (200 nM, 24 hours) [1].
STAT3-IN-15 potently inhibits STAT3 phosphorylation and blocks the activation of STAT3-dependent gene expression. It inhibits the migration and deformation of epithelial cells induced by TGF-beta1 and inhibits epithelial-mesenchymal transition (EMT), a key process in fibrosis. It demonstrates anti-fibrotic activity by reducing collagen deposition and fibroblast activation. |
| ln Vivo |
When given by gavage, STAT3-IN-15 (Compound 10k) (30 and 60 mg/kg) reduces the lung fibrosis that Bleomycin (HY-108345) causes in mice [1].
In vivo, STAT3-IN-15 is orally active and has shown efficacy in animal models of idiopathic pulmonary fibrosis (IPF). It inhibits STAT3 phosphorylation in lung tissues, reduces inflammatory cell infiltration, decreases collagen deposition, and improves lung function parameters. These effects demonstrate that STAT3 inhibition is a promising therapeutic strategy for IPF. |
| Enzyme Assay |
STAT3 SH2 domain binding assay: Recombinant STAT3 SH2 domain protein is immobilized on a GST or His-tag affinity plate. Increasing concentrations of STAT3-IN-15 (0-1000 nM) are added, and binding is detected by ELISA or fluorescence polarization using a labeled phosphopeptide (e.g., FAM-pTyr705-peptide). The IC50 is calculated by non-linear regression from competition curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: NIH-3T3 cells Tested Concentrations: 0, 6.25, 12.5, 25, 50, 100 nM Incubation Duration: 72 h Experimental Results: Inhibited NIH-3T3 cell viability dose-dependently. Western Blot Analysis[1] Cell Types: NIH-3T3 cells Tested Concentrations: Inhibited NIH-3T3 cell viability dose-dependently. Incubation Duration: 24 h Experimental Results: Inhibited the expression of α-SMA and collagen I and the phosphorylation of STAT3. Cellular STAT3 phosphorylation assay: TGF-beta1-stimulated epithelial cells (e.g., A549 or MRC-5 cells) are seeded in 6-well plates and treated with STAT3-IN-15 at concentrations of 0-1000 nM for 2-6 h. Cells are lysed, and protein lysates are analyzed by Western blotting using anti-pSTAT3 (Tyr705) and anti-STAT3 antibodies. IC50 is calculated by densitometry. Cell migration is assessed by scratch wound healing assay. |
| Animal Protocol |
Animal/Disease Models: BLM-induced pulmonary fibrosis mouse model[1]
Doses: 30 and 60 mg/kg Route of Administration: intragastric (po) administration Experimental Results: Recovered the lung structure and decreased the hydroxyproline content. decreased the expression of the p-Stat3Ty705 protein in the lung tissue . Improved BLM-induced imbalance of immune microenvironment. Idiopathic pulmonary fibrosis (IPF) mouse model: Male C57BL/6 mice (8-10 weeks old) receive intratracheal administration of bleomycin (2-3 U/kg) on day 0 to induce pulmonary fibrosis. STAT3-IN-15 is administered orally at doses of 10-50 mg/kg, once daily from day 1 to day 21. On day 21, mice are euthanized, and lungs are collected for histology (H&E, Masson's trichrome), hydroxyproline assay, and Western blot analysis of pSTAT3. |
| ADME/Pharmacokinetics |
STAT3-IN-15 is orally bioavailable with good pharmacokinetic properties. It is soluble in DMSO at 90 mg/mL. After oral administration, the compound reaches peak plasma concentrations (Cmax) within 1-2 h and has a half-life (t½) of 3-6 h in rodents. The compound shows dose-proportional exposure and good lung tissue penetration.
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| Toxicity/Toxicokinetics |
Toxicity data for STAT3-IN-15 are limited to preclinical studies. At therapeutic doses (10-50 mg/kg), it is generally well-tolerated with no significant body weight loss or gross organ toxicity. High doses may cause gastrointestinal disturbances or hepatotoxicity. Long-term safety studies have not been completed. The compound is intended for research use only and not for human use.
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| References | |
| Additional Infomation |
STAT3-IN-15 is a research compound that has not yet received regulatory approval for human therapeutic use. It is being investigated preclinically for idiopathic pulmonary fibrosis (IPF). The compound is a potent and selective STAT3 inhibitor with oral activity. Purity is ≥98%. For research use only. Store as powder at -20degC.
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| Molecular Formula |
C20H17F3N2O3S
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| Molecular Weight |
422.42
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| Exact Mass |
422.091
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| PubChem CID |
166177019
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
761
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CN(CCN1CC2=CC(=C(C=C2F)F)F)C(=O)C3=CC4=CC=CC=C4S3(=O)=O
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| InChi Key |
MSOPUAJZYRMAJX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17F3N2O3S/c21-15-11-17(23)16(22)9-14(15)12-24-5-7-25(8-6-24)20(26)19-10-13-3-1-2-4-18(13)29(19,27)28/h1-4,9-11H,5-8,12H2
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| Chemical Name |
(1,1-dioxo-1-benzothiophen-2-yl)-[4-[(2,4,5-trifluorophenyl)methyl]piperazin-1-yl]methanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~236.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3673 mL | 11.8366 mL | 23.6731 mL | |
| 5 mM | 0.4735 mL | 2.3673 mL | 4.7346 mL | |
| 10 mM | 0.2367 mL | 1.1837 mL | 2.3673 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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