79-6

A cell-permeable oxindole compound that selectively inhibits the transcriptional repression activity of BCL6 (by ~70% at 50 µM in 293T-based reporter assays), but not that of three other BTB/POZ (bric-a-brac tramtrack broad complex/Poxvirus zinc finger) family members, Kaiso, HIC1, and PLZF, by direct BCL6 binding (K_d = 138 µM) via the BTB domain and blocking corepressor BBD- (BCL6 binding domain) mediated BCL6 interaction (IC₅₀ = 212 µM & K_i = 147 µM in competitive binding against SMRT-BBD peptide), resulting in upregulation of BCL6 target genes in BCL-dependent DLBCL (diffuse large B cell lymphoma), but not BCL-independent Toledo and OCI-Ly4 cell lines. Shown to exhibit antiproliferative activity against DLBCL cell lines (IC₅₀ from 24 to 936 µM) as well as primary human DLBCL cells in vitro and suppress BCL-dependent tumor growth in mice (<40% of control tumor size on day 9; 50 mg/kg/day via i.p.) in vivo.

Packaged under inert gas

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

Cerchietti, L.C., et al. 2010. Cancer Cell17, 400.

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

Toxicity: Standard Handling (A)