|Solubility:||DMSO up to 10 mM|
|Chemical Name:||(Z)-2-(4-bromo-2-((4-oxo-3-(pyridin-3-ylmethyl)-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
SKPin C1 is a potent and selective inhibitor of Skp2-mediated p27 degradation. It selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts. In cancer cells, the compounds induced p27 accumulation in a Skp2-dependent manner and promoted cell-type-specific blocks in the G1 or G2/M phases. SKPin C1 is a useful chemical probe selectively targeting SCF-Skp2 protein-protein interface, may provide a new avenue of cancer treatment with enhanced specificity over Bortezomib.
How to Use:
- In vitro: SKPin C1 was used at 10 µM final concentration in various in vitro assays.
- In vivo: n/a
- Wu L, et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. (2012) Chem Biol. 19(12):1515-24.
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