STAT3-IN-17

• CAT Number: I024186
• CAS Number: 1245814-52-1
• Molecular Formula: C11H6F3N3O3S
• Molecular Weight: 317.24
• Purity: ≥95%
• Synonyms: N-(5-nitro-1,3-thiazol-2-yl)-4-(trifluoromethyl)benzamide
• InChI: InChI=1S/C11H6F3N3O3S/c12-11(13,14)7-3-1-6(2-4-7)9(18)16-10-15-5-8(21-10)17(19)20/h1-5H,(H,15,16,18)
• InChIKey: HKCGJKNZQDBZFT-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-])C(F)(F)F

STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori[1][2].
STAT3-IN-17 (compound 15) (10 μM; 20 h, 48 h) inhibits STAT3 pathway with inhibition rate of 76.5%, and also inhibits HEK-Blue IL-6 cells viability to 15%[1].
STAT3-IN-17 (2.5-40 μM; 24 h) inhibits the phosphorylation of STAT3 (Y705)[1].
STAT3-IN-17 (10 μM, 50 μM; 48 h) inhibits HEK 293T cell growth, as well as inhibiting HeLa cell growth with an IC50 value of 2.7 μM[1].
(D)-PPA 1 (compound 24) inhibits microorganisms Helicobacter pylori and Campylobacter jejuni with MIC values of 1.6 μM and 4.7 μM, respectively[2].
STAT3-IN-17 (compound 15) (5 mg/kg for ig, or 25 mg/kg for iv; single dose) exhibits greater pharmacokinetic properties than Nitazoxanide (HY-B0217) in rat, with a significantly longer half-life for elimination (t1/2β) (11.1 vs 0.8 h), greater absolute bioavailability (F) (87.4% vs 5.7%), and higher maximum plasma concentration (Cmax) (20.7 vs 1.0 mg/L) maximum plasma concentration (Cmax) (20.7 vs 1.0 mg/L)[1].

Reference

[1]. Lü Z, et al. Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors. ACS Med Chem Lett. 2021 Apr 1;12(5):696-703.
 [Content Brief]