SKP2 E3 Ligase Inhibitor IV – Calbiochem

Descrição detalhada : A cell-permeable dimethylanilinomethylamine compound that inhibits SKP2-dependent cellular p27Kip1 ubiquitination activity (10 to 30 microM; 16 h; in MM1.S myeloma and HeLa cultures) by preventing the incorporation of SKP2 into the Skp1-cullin1-F-box/SCF complex. Selectively induces the accumulation of known SCFSKP2 substrates (p21Cip1, p27Kip1, and p57Kip2) in multiple myeloma RPMI 8226 cells, without inducing HSP-27 phosphorylation or affecting cellular levels of Fbw7 and β-TrCP substrates (c-Jun and β-catenin, respectively) seen with proteasome inhibition by Bortezomib (Cat. No. 504314) treatment. Shown to exhibit antiproliferation activity against 13 myeloma lines (GI50 in 3 d from 4.2 to 13.2 microM), including melphalan-, doxorubicin- and steroid-resistant clones, via autophage-initiated cell death induction in a caspase-3-independent manner, and exhibit cancer-selective cytotoxicity against primary CD138+ malignant cells vs. CD138- nonneoplastic blood cells from MM patient blood (viability in 24 h with/without 5 microM drug treatment = 1.38%/66.4% for CD138+ vs. 81.3%/94% CD138-)., A cell-permeable dimethylanilinomethylamine compound that inhibits SKP2-dependent p27Kip1 ubiquitination (10 to 30 microM; 16 h; in MM1.S myeloma and HeLa cultures) by preventing the incorporation of SKP2 into the Skp1-cullin1-F-box/SCF complex. Selectively induces the accumulation SCFSKP2 substrates in multiple myeloma RPMI 8226 cells without affecting cellular levels of Fbw7 or β-TrCP substrate (c-Jun and β-catenin, respectively) seen with proteasome inhibition by Bortezomib (Cat. No. 504314) treatment. Shown to exhibit cancer-selective cytotoxicity against primary CD138+ malignant cells over CD138- nonneoplastic blood cells from MM patient blood (viability in 24 h with/without 5 microM drug treatment = 1.38%/66.4% for CD138+ vs. 81.3%/94% CD138-).
Sinónimos : SKP2 E3 Ligase Inhibitor IV - Calbiochem; CRL1 SKP2 Inhibitor IV, p21/Cip1/Waf1 Activator IV, p27/Kip1 Activator IV, S-phase Kinase-associated Protein 2 Inhibitor IV; SCF SKP2 Inhibitor IV, (+/-)-4-((3-(2,2-Dimethyltetrahydro-2H-pyran-4-yl)-4-phenylbutylamino)methyl)-N,N
Fórmula molecula r: C26H38N2O · 2HCl
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA