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| | P 22077 Basic information |
| Product Name: | P 22077 | | Synonyms: | P 22077;1-(5-(2,4-difluorophenylthio)-4-nitrothiophen-2-yl)ethanone;1-[5-[(2,4-Difluorophenyl)thio]-4-n-itro-2-thienyl]-ethanone;Ethanone, 1-[5-[(2,4-difluorophenyl)thio]-4-nitro-2-thienyl]-;1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]ethanone P 22077;P 22077 1-[5-[(2,4-Difluorophenyl)thio]-4-nitro-2-thienyl]ethanone;1-[5-(2,4-Difluoro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone;CS-1115 | | CAS: | 1247819-59-5 | | MF: | C12H7F2NO3S2 | | MW: | 315.32 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1247819-59-5.mol |  |
| | P 22077 Chemical Properties |
| Melting point | 146 - 148°C | | Boiling point | 395.4±42.0 °C(Predicted) | | density | 1.53±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to 25 mg/ml) | | form | solid | | color | Off-white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| | P 22077 Usage And Synthesis |
| Description | P22077 (1247819-59-5) is a selective (tested against 23 other DUBs) inhibitor of USP7 (IC50?= 8 μM) and the closely related USP47.1,2?It destabilizes claspin, a scaffolding protein involved in regulating Chk1 kinase, a DNA damage response enzyme.2?P22077 inhibits neuroblastoma growth?via?induction of p53-mediated apoptosis.3?N-Myc was destabilized by P22077 inhibition of USP7 in human neuroblastoma cells.4?It was able to stabilize p53 levels in conjunction with an Mdm2 inhibitor (Nutlin-3,?Cat# 10-1350)?in HCT116 colorectal carcinoma cells.5 | | Uses | P22077 is an analog of the ubiquitin-specific protease (USP7) inhibitor P5091. It inhibits USP7, as well. | | storage | Store at +4°C | | References | 1) Tian?et al. (2011),?Characterization of Selective Ubiquitin and Ubiquitin-like Protease Inhibitors Using a Fluorescence-Based Multiplex Assay Format; Assay Drug Dev. Technol.?9?165
2) Altun?et al.?(2011),?Activity-based chemical proteomics accelerates inhibitor development for deubiquitinylating enzymes; Chem. Biol.?18?1401
3) Fan?et al.?(2013),?USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis;?Cell Death Dis.?4?e867
4) Tavana?et al.?(2016),?HAUSP deubiquitinates and stabilizes M-Myc in neuroblastoma; Nat. Med.?22?1180
5) Tavana?et al.?(2018),?Targeting HAUSP in both p53 wildtype and p53-mutant tumors; Cell Cycle?17?823 |
| | P 22077 Preparation Products And Raw materials |
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