STAT3-IN-15

• CAT Number: I042380
• Molecular Formula: C20H17F3N2O3S
• Molecular Weight: 422.42
• Purity: ≥95%
• Synonyms: (1,1-dioxo-1-benzothiophen-2-yl)-[4-[(2,4,5-trifluorophenyl)methyl]piperazin-1-yl]methanone
• InChI: 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
• InChIKey: MSOPUAJZYRMAJX-UHFFFAOYSA-N
• SMILES: C1CN(CCN1CC2=CC(=C(C=C2F)F)F)C(=O)C3=CC4=CC=CC=C4S3(=O)=O

STAT3-IN-15 is a potent and orally active STAT3 inhibitor against idiopathic pulmonary fibrosis (IPF). STAT3-IN-15 inhibits STAT3 phosphorylation. STAT3-IN-15 also inhibits the migration and deformation of epithelial cells induced by TGF-β1 and inhibit epithelial-mesenchymal transition (EMT)[1].
STAT3-IN-15 (compound 10k) inhibits NIH-3T3 cell proliferation with an IC50 of 0.47 μM[1].
STAT3-IN-15 forms hydrogen bonds with Lys591 and Ser636, occupying the pY subpocket of STAT3[1].
STAT3-IN-15 (0-100 nM, 72 h) inhibits fibroblast activation and proliferation[1].
STAT3-IN-15 (50 nM, 24 h) inhibited TGF-β1 (5 ng/mL)-induced activation of NIH-3T3 cells[1].
STAT3-IN-15 (200 nM, 24 h) blocks TGF-β1 induced EMT process in A549 cells, determined by morphological changes[1].
STAT3-IN-15 (compound 10k) (30 and 60 mg/kg, intragastric administration) alleviates Bleomycin.html” class=”link-product” target=”_blank”> Bleomycin (HY-108345)-induced pulmonary fibrosis in mouse[1].

Reference

[1]. Wang Y, et al. Discovery of the novel Benzo[b]thiophene 1,1-dioxide derivatives as a potent STAT3 inhibitor against idiopathic pulmonary fibrosis. Eur J Med Chem. 2022 Nov 28;246:114953.
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