Product Information
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.

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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Proteases Inhibitors > Proteasome and Ubiquitination Pathway Inhibitors