882257-11-6

Basic information

• Product Name: P-5091
• Synonyms: 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitro-2-thienyl]ethanone;P5091, >=98%;1-[5-(2,3-Dichloro-phenylsulfanyl)-4-nitro-thiophen-2-yl]-ethanone;P 005091;P 5091;P005091;P-005091;P5091
• CAS NO: 882257-11-6
• Molecular Formula: C₁₂H₇Cl₂NO₃S₂
• Molecular Weight: 348.22488
• Product Categories: Inhibitors
• Mol File: 882257-11-6.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 452.4±45.0 °C(Predicted)
• Appearance: light yellow to dark yellow/
• Density: 1.60±0.1 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• Solubility: DMSO: soluble10mg/mL, clear
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
• CAS DataBase Reference: P-5091(CAS DataBase Reference)
• NIST Chemistry Reference: P-5091(882257-11-6)
• EPA Substance Registry System: P-5091(882257-11-6)

Safety Data

• Hazard Codes: T
• Statements: 25
• Safety Statements: 45
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: 3
• Hazardous Substances Data: 882257-11-6(Hazardous Substances Data)

Usage

Description

P5091 (882257-11-6) is a selective inhibitor of the ubiquitin-specific protease USP7 ( IC50=4.2 μM).1,2 Induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.1?P5091 displays antiangiogenic activity in vivo.2?Cell permeable

Uses

Different sources of media describe the Uses of 882257-11-6 differently. You can refer to the following data:
1. P005091 is a selective dual inhibitor of the cancer-related deubiquitylating proteases USP7 and USP47.
2. P5091 has been used:as a ubiquitin specific peptidase 47 (USP47) inhibitor in 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to evaluate the cellular viability of MCF-10A cellsas a USP7 inhibitor to study the regulatory role for USP7 on inflammasome activationas USP7 inhibitor in drug susceptibility assays to study its effect on bone marrow?resident tumor cells (BMRTCs)/ circulating tumor cells (CTCs)

Biochem/physiol Actions

P5091 plays an important role in ovarian cancer, as it can prevent the growth of cells and can promote necrosis and apoptosis.

References

1) Chauhan et al. (2012), A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance; Cancer Cell, 22 345 2) Weinstock et al. (2012), Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47; ACS Med. Chem. Lett., 3 789

Upstream product

• 6310-09-4 2-acetyl-5-chlorothiophene 
• 42456-75-7 5-acetyl-2-chloro-3-nitrothiophene 
• 17231-95-7 2,3-dichlorobenzenethiol 

Downstream Products

• 1247819-83-5 1-[5-(2,3-dichlorophenyl)sulfanyl-4-nitro-2-thienyl]ethanol 

Relevant articles and documents

Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47

Inhibitors of the cancer-related cysteine isopeptidase human ubiquitin-specific proteases 7 (USP7) and 47 (USP47) are considered to have potential as cancer therapeutics, owing to their ability to stabilize the tumor suppressor p53 and to decrease DNA polymerase β(Polβ), both of which are potential anticancer effects. A new class of dual small molecule inhibitors of these enzymes has been discovered. Compound 1, a selective inhibitor of USP7 and USP47 with moderate potency, demonstrates inhibition of USP7 in cells and induces elevated p53 and apoptosis in cancer cell lines. Compound 1 has been shown to demonstrate modest activity in human xenograft multiple myeloma and B-cell leukemia in vivo models. This activity may be the result of dual inhibition of USP7 and USP47. To address issues regarding potency and developability, analogues of compound 1 have been synthesized and tested, leading to improvements in potency, solubility, and metabolic reactivity profile. Further optimization is expected to yield preclinical candidates and, ultimately, clinical candidates for the treatment of multiple myeloma, prostate cancer, and other cancers.