STAT3 Inhibitor XIII, C188-9-Calbiochem

C₂₇H₂₁NO₅S

471.52

MFCD03141581

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.
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.

Toxicity: Toxic (F)

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

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

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

100

≥98% (HPLC)

powder

Calbiochem^®

OK to freeze
protect from light

off-white to pale beige

DMSO: 100 mg/mL

ambient

2-8℃

OC1=C(C2=C(O)C=CC3=C2C=CC=C3)C=C(NS(C(C=C4)=CC=C4OC)(=O)=O)C5=C1C=CC=C5

10 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3