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530236 SKP2 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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: Skp1/Skp2 interaction
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530236
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
634908-46-6C₂₆H₃₈N₂O • 2HCl

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      Description
      OverviewA 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 Number530236
      Brand Family Calbiochem®
      SynonymsCRL1SKP2 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
      ReferencesChen, Q., et al. 2008. Blood 111, 4690.
      Product Information
      CAS number634908-46-6
      FormWhite solid
      Hill FormulaC₂₆H₃₈N₂O • 2HCl
      Chemical formulaC₂₆H₃₈N₂O • 2HCl
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSkp1/Skp2 interaction
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      5.30236.0001 04055977261318

      Documentation

      SKP2 E3 Ligase Inhibitor IV - CAS 634908-46-6 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Chen, Q., et al. 2008. Blood 111, 4690.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision18-April-2014 JSW
      SynonymsCRL1SKP2 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
      DescriptionA cell-permeable dimethylanilinomethylamine compound that inhibits SKP2-dependent cellular p27Kip1 ubiquitination activity (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 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 µM), 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 µM drug treatment = 1.38%/66.4% for CD138+ vs. 81.3%/94% CD138-).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number634908-46-6
      Chemical formulaC₂₆H₃₈N₂O • 2HCl
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesChen, Q., et al. 2008. Blood 111, 4690.