530236 SKP2 E3 Ligase Inhibitor IV - Calbiochem

530236
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₆H₃₈N₂O • 2HCl

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30236.0001
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          Glass bottle 10 mg
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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
          FormWhite solid
          Hill FormulaC₂₆H₃₈N₂O • 2HCl
          Chemical formulaC₂₆H₃₈N₂O • 2HCl
          ReversibleY
          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

          Documentation

          SKP2 E3 Ligase Inhibitor IV - 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
          Chemical formulaC₂₆H₃₈N₂O • 2HCl
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesChen, Q., et al. 2008. Blood 111, 4690.