详情描述
P22077 is a potent and selective USP7 inhibitor that was recently identified using an Ub-CHOP reporter assay. It was shown to have potent and selective inhibitory activity against USP7 and closely related USP47 at ~5 µM, but not other DUBs (at ~15-45 µM). USP7, also known as HAUSP, plays an important role in cancer progression as it affects the stability of p53. The inhibition of USP7 is predicted to destabilize HDM2 and stabilize p53, and USP7 exerts both p53-dependent and p53-independent effects on controlling cell proliferation and apoptosis.
Product information
CAS Number: 1247819-59-5
Molecular Weight: 315.32
Formula: C12H7F2NO3S2
Chemical Name: 1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
Smiles: CC(=O)C1=CC(=C(SC2=CC=C(F)C=C2F)S1)[N+]([O-])=O
InChiKey: RMAMGGNACJHXHO-UHFFFAOYSA-N
InChi: InChI=1S/C12H7F2NO3S2/c1-6(16)11-5-9(15(17)18)12(20-11)19-10-3-2-7(13)4-8(10)14/h2-5H,1H3
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100mM
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:
P22077 was used at 25 µM in vitro and in cells.
References:
- Nicholson B, et al. The multifaceted roles of USP7: new therapeutic opportunities. (2011) Cell Biochem Biophys. 60(1-2):61-8.
- Mikael Altun et al. Activity-Based Chemical Proteomics Accelerates Inhibitor Development for Deubiquitylating Enzymes. (2011) Chemistry & Biology 18, 1401–1412.
Products are for research use only. Not for human use.