P5091 (P005091)

For research use only.

Catalog No.S7132

34 publications

P5091 (P005091) Chemical Structure

CAS No. 882257-11-6

P5091(P005091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.

Selleck's P5091 (P005091) has been cited by 34 publications

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Biological Activity

Description P5091(P005091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM and the closely related USP47.
USP7 [1]
(Cell-free assay)
USP47 [2]
(Cell-free assay)
4.2 μM(EC50) 4.3 μM
In vitro

P5091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P5091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P5091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P5091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P5091. Moreover, P5091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P5091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P5091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P5091 inhibits growth in MM cells and overcomes bortezomib-resistance. P5091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6–14 μM). P5091 overcomes bone marrow stromal cell-induced growth of MM Cells. P5091 decreased HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, 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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Ml\uSpVv[3Srb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IGXTVFch\XiycnXzd4VlKGmwIGPmPUBk\WyuczDifUBW[i2FSF;QJJJmeG:{dHXyJIF{e2G7LDDFR|UxRTRwMjFOwG0> NV60SWtrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA{QDFpPkK0PVAxOzhzPD;hQi=>
human HCT116 cells NWTEUpp6S3m2b4TvfIlkyqCjc4PhfS=> MmjPO|IhcA>? M2TkUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOsJGVEPTB;MUGg{txO NUnZRndqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA{QDFpPkK0PVAxOzhzPD;hQi=>
multiple myeloma cells NHu3eWZHfW6ldHnvckBie3OjeR?= M4jM[GlvcGmkaYTpc44hd2ZiVWPQO{BqdiCvdXz0bZBt\SCveXXsc41iKGOnbHzzJEh2dmuwb4fuJI9zcWerbjmgZpkhcW2vdX7vbIl{fG:laHXtbZN1enluIFXDOVAhRSB2LkKg{txONg>? NGHyVoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO2OFg3Pyd-MkWzOlQ5Pjd:L3G+
Sf9 MlLISpVv[3Srb36gZZN{[Xl? NVq0bnBYOzBibXnudy=> MX3Jcohq[mm2aX;uJI9nKG[3bHytcIVv\3SqIILlZ49u[mmwYX70JHVUWDdiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJV{cW6pIGXiMWVMVCCjczDzeYJ{fHKjdHWgdJJmcW6ldXLheIVlKG[xcjCzNEBucW6|IH\vcIxwf2WmIHL5JJN2[nO2cnH0[UBi\GSrdHnvckBjgSCobIXvdoV{[2WwY3WgZoF{\WRiYYPzZZktKEmFNUCgQUA1NjJizszNMi=> NFX2W4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe2PFExOid-Mki3OlgyODJ:L3G+

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
HAUSP / N-Myc; 

PubMed: 29616860     

Extracts of SK-N-DZ cells treated with DMSO or a serial titration of p5091 from 25 µm-3.125 µm for 8 h and immunoblotted with antibodies specific for HAUSP, N-Myc, and Actin. 

USP7 / p53 / p21; 

PubMed: 30045945     

Western blots showing increase in p53 and p21 protein levels with P5091 treatment in TP53 wild-type Ewing sarcoma cell lines.

29616860 30045945

PubMed: 28418900     

Immunofluorescence assay showing PTEN cellular compartmentalization in MEC-1 cells treated with 4.2 μM P5091 for 24 hours. Anti-PTEN antibody (green); Propidium iodide (red). 

Growth inhibition assay
Cell viability; 

PubMed: 30045945     

(B) Ewing sarcoma cells were treated with P5091 for 3 d. TP53 wild-type Ewing sarcoma cell lines are shown in red; TP53 mutant Ewing sarcoma cell lines are shown in black. Values were normalized to vehicle controls. Each data point shows the mean of eight replicates; error bars are mean values ± standard deviation. The experiment was performed twice and data points of one representative experiment are shown. 

In vivo In animal tumor model studies, P5091 is well tolerated, inhibits tumor growth, and prolongs survival. Combining P5091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggers synergistic anti-MM activity. [1]


Animal Research:


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  • Animal Models: CB-17 SCID-mice
  • Dosages: 10 mg/kg
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 28 mg/mL (80.4 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 400+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 348.22


CAS No. 882257-11-6
Storage powder
in solvent
Synonyms N/A
Smiles CC(=O)C1=CC(=C(S1)SC2=C(C(=CC=C2)Cl)Cl)[N+](=O)[O-]

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DUB Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID