530236 Sigma-AldrichSKP2 E3 Ligase Inhibitor IV - CAS 634908-46-6 - Calbiochem
A cell-permeable inhibitor of SKP2-dependent p27Kip1 ubiquitination. Selectively induces the accumulation SCFSKP2 substrates in multiple myeloma RPMI 8226 cells.
More>> A cell-permeable inhibitor of SKP2-dependent p27Kip1 ubiquitination. Selectively induces the accumulation SCFSKP2 substrates in multiple myeloma RPMI 8226 cells. Less<<Synonyms: CRL1SKP2 Inhibitor IV, p21/Cip1/Waf1 Activator IV, p27/Kip1 Activator IV, S-phase Kinase-associated Protein 2 Inhibitor IV; SCFSKP2 Inhibitor IV, (±)-4-((3-(2,2-Dimethyltetrahydro-2H-pyran-4-yl)-4-phenylbutylamino)methyl)-N,N-dimethylaniline, 2HCl
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Overview
Key Spec Table
CAS # | Empirical Formula |
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634908-46-6 | C₂₆H₃₈N₂O • 2HCl |
Products
Catalogue Number | Packaging | Qty/Pack | |
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5.30236.0001 | Sklená flaša | 10 mg |
Description | |
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Overview | A cell-permeable dimethylanilinomethylamine compound that inhibits SKP2-dependent p27Kip1 ubiquitination (10 to 30 µM; 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 µM drug treatment = 1.38%/66.4% for CD138+ vs. 81.3%/94% CD138-). |
Catalogue Number | 530236 |
Brand Family | Calbiochem® |
Synonyms | CRL1SKP2 Inhibitor IV, p21/Cip1/Waf1 Activator IV, p27/Kip1 Activator IV, S-phase Kinase-associated Protein 2 Inhibitor IV; SCFSKP2 Inhibitor IV, (±)-4-((3-(2,2-Dimethyltetrahydro-2H-pyran-4-yl)-4-phenylbutylamino)methyl)-N,N-dimethylaniline, 2HCl |
References | |
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References | Chen, Q., et al. 2008. Blood 111, 4690. |
Product Information | |
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CAS number | 634908-46-6 |
Form | White solid |
Hill Formula | C₂₆H₃₈N₂O • 2HCl |
Chemical formula | C₂₆H₃₈N₂O • 2HCl |
Reversible | Y |
Quality Level | MQ100 |
Biological Information | |
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Primary Target | Skp1/Skp2 interaction |
Purity | ≥95% by HPLC |
Physicochemical Information | |
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Cell permeable | Y |
Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
Global Trade Item Number | |
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Catalogue Number | GTIN |
5.30236.0001 | 04055977261318 |