882257-11-6 Usage
Description
P-5091 is a selective dual inhibitor of the cancer-related deubiquitylating proteases USP7 and USP47, characterized by its ability to induce apoptosis in multiple myeloma cells, overcome bortezomib resistance, and display antiangiogenic activity in vivo. It is a cell permeable compound with an IC50 of 4.2 μM for USP7 inhibition.
Uses
Used in Cancer Research:
P-5091 is used as a ubiquitin-specific peptidase 47 (USP47) inhibitor in the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay to evaluate the cellular viability of MCF-10A cells. It is also used as a USP7 inhibitor to study the regulatory role of USP7 on inflammasome activation and its effect on bone marrow resident tumor cells (BMRTCs) and circulating tumor cells (CTCs) in drug susceptibility assays.
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
Check Digit Verification of cas no
The CAS Registry Mumber 882257-11-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,8,2,2,5 and 7 respectively; the second part has 2 digits, 1 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 882257-11:
(8*8)+(7*8)+(6*2)+(5*2)+(4*5)+(3*7)+(2*1)+(1*1)=186
186 % 10 = 6
So 882257-11-6 is a valid CAS Registry Number.
882257-11-6Relevant articles and documents
Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47
Weinstock, Joseph,Wu, Jian,Cao, Ping,Kingsbury, William D.,McDermott, Jeffrey L.,Kodrasov, Matthew P.,McKelvey, Devin M.,Suresh Kumar, K. G.,Goldenberg, Seth J.,Mattern, Michael R.,Nicholson, Benjamin
, p. 789 - 792,4 (2020/09/15)
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.