General description
A cell-permeable binaphthol-sulfonamide that competes against pY proteins for Stat3 SH2 domain binding. Shown to inhibit G-CSF-induced (100 ng/ml for 15 min following 1 h drug pretreatment) Stat3 tyr705 phosphorylation in 6 human AML cell lines (IC50 from 4.1 to 8.3 µM) and 4 primary pediatric AML cultures (IC50 from 8 to 18 µM). Long-term treatments (24 h for lines and 48 h for primary cultures) result in apoptosis induction (Annexin V-PE staining) in 7 AML lines (EC50 from 8.4 to 43.6 µM) and CD34+ populations from 5 primary pediatric AML samples (EC50 from 0.8 to25 µM). Selectivity studies using Kasumi-1 cells reveals concomitant inhibitions of G-CSF-stimulated TIE2, MATK, JAK1, and HGFR phosphorylation (by 90%, 50%, 40%, and 40%, respectively; 10 µM C188-9), but not 15 other phosphoproteins (≤30% inhibition), including pERK1/2 and pAKT.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Redell, M.S., et al. 2011. Blood112, 355.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Toxic (F)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white to pale beige |
| solubility | DMSO: 100 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | OC1=C(C2=C(O)C=CC3=C2C=CC=C3)C=C(NS(C(C=C4)=CC=C4OC)(=O)=O)C5=C1C=CC=C5 |
| InChI key | QDCJDYWGYVPBDO-UHFFFAOYSA-N |
