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 (Kd = 138 µM) via the BTB domain and blocking corepressor BBD- (BCL6 binding domain) mediated BCL6 interaction (IC50 = 212 µM & Ki = 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.
Confezionamento
Packaged under inert gas
Attenzione
Toxicity: Standard Handling (A)
Ricostituzione
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Altre note
Cerchietti, L.C., et al. 2010. Cancer Cell17, 400.
Note legali
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
Certificati d'analisi (COA)
Cerca il Certificati d'analisi (COA) digitando il numero di lotto/batch corrispondente. I numeri di lotto o di batch sono stampati sull'etichetta dei prodotti dopo la parola ‘Lotto’ o ‘Batch’.
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