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SKPin C1, Skp2 Inhibitor

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SKPin C1, Skp2 Inhibitor

$109.00
A potent and selective inhibitor of Skp2-mediated p27 degradation.
Catalog No. Unit Price Qty
M60137-2s 2 mg solid $109.00

Details

Product Information
Molecular Weight: 465.34
Formula: C18H13BrN2O4S2
Purity: ≥98%
CAS#: 432001-69-9
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.

Biological Activity:

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


Reference:

  1. 1. Wu L, et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. (2012) Chem Biol. 19(12):1515-24.


Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 465.34
Formula: C18H13BrN2O4S2
Purity: ≥98%
CAS#: 432001-69-9
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.

Biological Activity:

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


Reference:

  1. 1. Wu L, et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. (2012) Chem Biol. 19(12):1515-24.


Products are for research use only. Not for human use.

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