P22077

Catalog No.S7133

P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.

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P22077 Chemical Structure

P22077 Chemical Structure
Molecular Weight: 315.32

Validation & Quality Control

Quality Control & MSDS

Product Information

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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description P22077 is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM, also inhibits the closely related USP47.
Targets USP7 [1] USP47 [2] USP2 core [2] USP4 [2]

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IC50 8.6 μM(EC50) 8.74 μM(EC50) >50 μM(EC50) >50 μM(EC50)
In vitro P22077 is an analog of the recently discovered USP7 inhibitor P5091. P22077 has negligible activity versus DEN1 and SENP2core over the concentration range tested, but inhibits USP7 with an IC50 of 8 μM. [1] The inhibitory activities of P22077 in vitro against a panel of DUBs, cysteine proteases, and other families of proteolytic enzymes demonstrate that P22077 inhibits USP7 and the closely related DUB USP47. P22077 inhibits a smaller subset of DUBs at a concentration of 15–45 mM in cell lysates. P22077 induces (tumor) cell death with EC50 values in the low micromolar range. P22077 inhibition exhibited changes in ubiquitylated protein levels that are distinct from the broad specificity inhibitor. P22077 treatment of U2OS cells during release from G1/S arrest induces with hydroxyurea resulted in a dose-dependent loss of claspin protein and a concomitant decrease in phospho Serine 317 Chk1. Furthermore, quantitative MS suggestes the E3 ubiquitin ligase components RBX1, DCAF7, DCAF11, and the DNA damage binding protein 1 (DDB1) to be reduced upon cellular treatment with P22077. [2]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

UbL-EKL assays Unless stated otherwise, recombinant isopeptidase is mixed with UbL-EKL and EKLsubstrate I to final concentrations of 20, 50, and 20 nM, respectively, in a total volume of 100 μL in a well in a black-walled 96-well plate. All dilutions are performed in isopeptidase assay buffer (20 mM Tris-HCl, pH 8.0, 2 mM CaCl2, and 2 mM β-mercaptoethanol). The increase in fluorescence intensity over time is determined on a Perkin Elmer Envision fluorescence plate reader with excitation and emission filters corresponding to the fluorescence resonance energy transfer peptide utilized. Unless stated otherwise, net relative fluorescence units (RFUs) are determined by subtracting the blank RFU value (20 nM EKL substrate I or 100 nM EKL substrate II in isopeptidase assay buffer) from each data point. SENP2core, SUMO3-EKL sensitivity experiments are performed by mixing 0–100 fM SENP2core with 50 nM SUMO3-EKL, and 100 nM EKL substrate I in a total volume of 100 μL as above.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tian X, et al. Assay Drug Dev Technol, 2011, 9(2), 165-173.

[2] Altun M, et al. Chem Biol, 2011, 18(11), 1401-1412.

Chemical Information

Download P22077 SDF
Molecular Weight (MW) 315.32
Formula

C12H7F2NO3S2

CAS No. 1247819-59-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 63 mg/mL (199.79 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name Ethanone, 1-[5-[(2,4-difluorophenyl)thio]-4-nitro-2-thienyl]-

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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