STAT3-IN-11

• CAT Number: I043495
• CAS Number: 2503096-50-0
• Molecular Formula: C20H17NO4
• Molecular Weight: 335.35
• Purity: ≥95%
• Synonyms: N-[2-(8-hydroxy-3-methyl-1,4-dioxonaphthalen-2-yl)ethyl]benzamide
• InChI: InChI=1S/C20H17NO4/c1-12-14(10-11-21-20(25)13-6-3-2-4-7-13)19(24)17-15(18(12)23)8-5-9-16(17)22/h2-9,22H,10-11H2,1H3,(H,21,25)
• InChIKey: XLSYRTJOLUDGSR-UHFFFAOYSA-N
• SMILES: CC1=C(C(=O)C2=C(C1=O)C=CC=C2O)CCNC(=O)C3=CC=CC=C3

STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers[1].
STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells[1].
STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-1) [1].
STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the phosphorylation of STAT3 (stimulated by IL-6 in MDA-MB-231) at site pTyr705 in a dose-dependent manner[1].
STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the expression of the downstream gene (Survivin and Mcl-1) of STAT3 in a concentration-dependent manner[1].
STAT3-IN-11 (2.5-10 μM, 6 h) has no effects on the typical upstream kinases of STAT3 such as p-JAK2 and p-Src and the phosphorylation of STAT1 (a STAT isoform) [1].
STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner[1].

Reference

[1]. Li N, et al. Design, synthesis and biological evaluation of novel plumbagin derivatives as potent antitumor agents with STAT3 inhibition. Bioorg Chem. 2020 Nov;104:104208.
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