A cell-permeable binaphthol-sulfonamide compound that competitively disrupts Stat3 SH2 domain-pY peptide interaction and acts as a reversible inhibitor of Stat3 activation and Stat3-dependent gene transcription. Shown to block G-CSF stimulated pStat3 (IC50=4.1, 4.5 and 8.3uM in KG-1, Kasumi-1 and NB-4 cells, respectively), with no effect on ligand-induced pStat1 and selectively induce apoptosis of Stat3-dependent AML cells ((EC50 of 6-8uM) and growth arrest. Moderately affects Tie2 kinase activity (<50%) with minimal effect on JAK1, JAK2, Src family kinases and pERK1/2 and pAKT at 10uM. Formula: C27H21NO5S Molecular Weight: 471.5 Solubility: DMSO (100mg/ml) (Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular Weight:
471.5
Purity:
98% (HPLC)
Form:
Supplied as an off-white to pale beige powder.
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