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.
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Autres remarques
Cerchietti, L.C., et al. 2010. Cancer Cell17, 400.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Certificats d'analyse (COA)
Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".
Déjà en possession de ce produit ?
Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.
The Journal of clinical investigation, 134(15) (2024-08-01)
Inflammatory neuropathies, which include chronic inflammatory demyelinating polyneuropathy (CIDP) and Guillain Barré syndrome (GBS), result from autoimmune destruction of the PNS and are characterized by progressive weakness and sensory loss. CD4+ T cells play a key role in the autoimmune
Antibiotic-resistant bacteria are a major global health threat that continues to rise due to a lack of effective vaccines. Of concern are Klebsiella pneumoniae that fail to induce in vivo germinal center B cell responses, which facilitate antibody production to
Cancer immunology research, 8(5), 698-709 (2020-03-04)
Although treatment with the glucocorticoid-induced tumor necrosis factor receptor-related protein (GITR) agonistic antibody (DTA-1) has shown antitumor activity in various tumor models, the underlying mechanism is not fully understood. Here, we demonstrate that interleukin (IL)-21-producing follicular helper T (Tfh) cells
Questions
Reviews
★★★★★ No rating value
Active Filters
Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..
