General description

A cell-permeable binaphthol-sulfonamide that competes against pY proteins for Stat3 SH2 domain binding. Shown to inhibit G-CSF-induced Stat3 tyr705 phosphorylation in human AML cell lines and primary cultures (IC₅₀ from 4.1 to 18 µM). Also shown to inhibit 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, in Kasumi-1 cells.

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.

Legal Information

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

Other Notes

Redell, M.S., et al. 2011. Blood112, 355.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Toxic (F)