573125

STAT3 Inhibitor IX, Cpd188

The STAT3 Inhibitor IX, Cpd188, also referenced under CAS 823828-18-8, controls the biological activity of STAT3.

• Synonym(s): STAT3 Inhibitor IX, Cpd188, 4-((3-(Carboxymethylsulfanyl)-4-hydroxy-1-naphthyl)sulfamoyl)benzoic acid
• Empirical Formula (Hill Notation): C₁₉H₁₅NO₇S₂
• CAS Number: 823828-18-8
• Molecular Weight: 433.45
• MDL number: MFCD05804524
• UNSPSC Code: 12352200
• NACRES: NA.28
• Assay: ≥90% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥90% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: beige
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [S](=O)(=O)(Nc2c3c(c(c(c2)SCC(=O)O)O)cccc3)c1ccc(cc1)C(=O)O
• InChI: 1S/C19H15NO7S2/c21-17(22)10-28-16-9-15(13-3-1-2-4-14(13)18(16)23)20-29(26,27)12-7-5-11(6-8-12)19(24)25/h1-9,20,23H,10H2,(H,21,22)(H,24,25)
• InChI key: CIERPRDYPKVDJO-UHFFFAOYSA-N

Description

General description

A cell-permeable naphthol compound that inhibits IL-6-stimulated STAT3 Tyr⁷⁰⁵ phosphorylation and nuclear translocation in HepG2 cells (IC₅₀ = 73 and 39 µM, respectively) by targeting STAT3 SH2 domain peptide-binding pocket (IC₅₀ = 20 µM against EGFR-derived pY-peptide binding), while exhibiting little effect against IFN-γ-stimulated HepG2 cellular STAT1 phosphorylation even at concentrations as high as 300 µM. Shown to preferentially induce apoptosis in cultures expressing constitutively active STAT3 (EC₅₀ = 0.73, 3.96, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively), while being less effective against cells without constitutively active STAT3 (EC₅₀ = 15.5 and 17.19 µM in MDA-MB-453 and MCF7 cultures, respectively).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Xu, X., et al. 2009. PLoS One4, e4783.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable