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P5091

Cat. No. M2195
P5091 Structure
Synonym:

P005091

Size Price Availability Quantity
10mg USD 98 In stock
50mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Customer Product Validations & Biological Datas
Source Int J Mol Sci (2017). Figure 3. P5091
Method cell proliferation assay
Cell Lines ovarian cancer cell
Concentrations 50 μM
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 348.22
Formula C12H7Cl2NO3S2
CAS Number 882257-11-6
Purity >98%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: P5091, P005091 supplier, Deubiquitinase, inhibitors

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