详情描述
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.
Product information
CAS Number: 432001-69-9
Molecular Weight: 465.34
Formula: C18H13BrN2O4S2
Chemical Name: (Z)-2-(4-bromo-2-((4-oxo-3-(pyridin-3-ylmethyl)-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid
Smiles: OC(=O)COC1=CC=C(Br)C=C1/C=C1\SC(=S)N(CC2C=CC=NC=2)C\1=O
InChiKey: IYCJJVVXEHZJHE-CHHVJCJISA-N
InChi: InChI=1S/C18H13BrN2O4S2/c19-13-3-4-14(25-10-16(22)23)12(6-13)7-15-17(24)21(18(26)27-15)9-11-2-1-5-20-8-11/h1-8H,9-10H2,(H,22,23)/b15-7-
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 10 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
SKPin C1 was used at 10 µM final concentration in various in vitro assays.
References:
- 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.