P5091 (P005091)

Catalog No.S7132

For research use only.

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.

P5091 (P005091) Chemical Structure

CAS No. 882257-11-6

Selleck's P5091 (P005091) has been cited by 36 publications

Purity & Quality Control

Choose Selective DUB Inhibitors

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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.
Targets
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 NV7P[HY{TnWwY4Tpc44h[XO|YYm= M33EfGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgWXNRPyCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KFWkLVPIU3AhemWyb4L0[ZIh[XO|YYmsJGVEPTB;ND6yJO69VQ>? NXnCW4EzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA{QDFpPkK0PVAxOzhzPD;hQi=>
human HCT116 cells MVfDfZRwfG:6aXRCpIF{e2G7 NUHXcVk{PzJiaB?= NVficYFQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{whTUN3ME2xNUDPxE1? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEO4NUc,OjR7MECzPFE9N2F-
multiple myeloma cells MWPGeY5kfGmxbjDhd5NigQ>? MkPQTY5pcWKrdHnvckBw\iCXU2C3JIlvKG23bITpdIxmKG27ZXzvcYEh[2WubIOgLJVvc26xd36gc5Jq\2mwKTDifUBqdW23bn;obZN1d2OqZX3pd5RzgSxiRVO1NEA:KDRwMjFOwG0v NGf5bm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO2OFg3Pyd-MkWzOlQ5Pjd:L3G+
Sf9 MU\GeY5kfGmxbjDhd5NigQ>? MVezNEBucW6| MoDTTY5pcWKrdHnvckBw\iCodXzsMYxmdme2aDDy[YNwdWKrbnHueEBWW1B5IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJHNnQSClZXzsd{B2e2mwZzDVZk1GU0xiYYOgd5Vje3S{YYTlJJBz\WmwY4XiZZRm\CCob4KgN|AhdWmwczDmc4xtd3enZDDifUB{fWK|dILheIUh[WSmaYTpc44h[nliZnz1c5Jme2OnbnPlJIJie2WmIHHzd4F6NCCLQ{WwJF0hPC5{IN88UU4> M{nU[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{[4NVAzLz5{OEe2PFExOjxxYU6=
Assay
Methods Test Index PMID
Western blot HAUSP / N-Myc ; USP7 / p53 / p21 29616860 30045945
Immunofluorescence PTEN 28418900
Growth inhibition assay Cell viability 30045945
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]

Protocol (from reference)

Animal Research:

[1]

  • 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.

5mg/mL

* 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
Formula

C12H7Cl2NO3S2

CAS No. 882257-11-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)C1=CC(=C(S1)SC2=C(C(=CC=C2)Cl)Cl)[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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