| Identification | Back Directory | [Name]
P 22077 | [CAS]
1247819-59-5 | [Synonyms]
P 22077
CS-1115
P 22077; P-22077
P 22077 USP/EP/BP
USP7/USP47 Inhibitor, 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-Difluoro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone
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 | [Molecular Formula]
C12H7F2NO3S2 | [MDL Number]
MFCD22580421 | [MOL File]
1247819-59-5.mol | [Molecular Weight]
315.316 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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. | [Enzyme inhibitor]
This ubiquitin cycle inhibitor (FW = 315.33 g/mol; CAS 1247819-59-5;
Solubility: 60 mg/mL DMSO), also known as 1-[5-[ (2,4-
difluorophenyl) thio]-4-nitro-2-thienyl]ethanone, targets Ubiquitin-Specific
Peptidase-7 (or USP-7) with an EC50 value of 8.6 μM. P22077 also inhibits
the structurally related peptidase USP-47. | [in vivo]
P 22077 (15 mg/kg, i.p. 21 days) shows potent antitumor activities in an xenograft mouse model bearing IMR-32-derived tumors; P 22077 also exhibits antitumor effects after treatment at 10 mg/kg for 14 days in mice bearing SH-SY5Y-derived tumors, and at 20 mg/kg for 12 days in mice bearing NGP-derived tumors[2]. | [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 |
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