P5091 (P005091) is a cell permeable, potent and specific inhibitor of deubiquitylating enzyme USP7, which induces elevated p53 and apoptosis in cancer cell lines. P5091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P5091 treatment, the cytotoxic activity of P5091 is not dependent on p53. P5091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P5091 displays antiangiogenic activity in vivo. P5091 is well tolerated, inhibits tumor growth and prolongs survival in animal models of cancer.
|Source||Int J Mol Sci (2017). Figure 3. P5091|
|Method||cell proliferation assay|
|Cell Lines||ovarian cancer cell|
|Incubation Time||12 and 24 h|
|Results||At 12 and 24 hours, control cells treated with DMSO propagated healthily, while the growth of P5091 treated HeyA8 and OVCAR-8 cells was remarkably repressed, with some cells exhibiting rounded shapes or even detaching from the culture dish, indicative of cell death|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mg/mL|
A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance.
Chauhan D, et al. Cancer Cell. 2012 Sep 11;22(3):345-58. PMID: 22975377.
|Related Deubiquitinase Products|
PR-619 is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs) with EC50 of 1-20 μM.
b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
P22077 is a selective inhibitor of ubiquitin-specific protease (USP) 7 with EC50 of 8.6 μM.
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