Shopping Cart

Your shopping cart is currently empty

P005091

Name: P005091
Brand: TargetMol
SKU: T6925
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T6925Cas No. 882257-11-6

Alias P5091

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

P005091

Copy Product Info

🥰Excellent

Purity: 99.87%

Catalog No. T6925Alias P5091Cas No. 882257-11-6

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

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$39	In Stock	In Stock
5 mg	$63	In Stock	In Stock
10 mg	$81	In Stock	In Stock
25 mg	$158	In Stock	In Stock
50 mg	$270	In Stock	In Stock
100 mg	$432	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$68	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.87%

Color:White to Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.
Targets&IC50	USP7:4.2 μM
In vitro	P5091 demonstrates synergistic anti-multiple myeloma (anti-MM) activity when used in combination with Lenalidomide, the HDAC inhibitor SAHA, or Dexamethasone. In animal tumor models, P5091 is well-tolerated, inhibits tumor growth, and prolongs survival.
In vivo	P5091 exhibits potent, specific, and selective deubiquitinating (deubiquitinase) activity against USP7. Conversely, P5091 does not inhibit other tested DUBs or proteases from different families (EC50 >100 mM). It decreases HDM2 and HDMX levels while upregulating p53 and p21. P5091-induced cytotoxicity is partly mediated via the HDM2-p21 signaling axis, and despite the upregulation of p53 following P5091 treatment, its cytotoxic effects do not depend on p53. P5091 concentration-dependently inhibits USP7 tagged with HA-UbVME and dose-dependently inhibits USP7-mediated disassembly of ultra-high molecular weight ubiquitin chains. Moreover, P5091 inhibits the breakdown of polyK48-linked ubiquitin chains specifically by USP7 rather than USP2 or USP8. It suppresses USP7 deubiquitinase activity in MM cells without inhibiting protease activities and overcomes bone marrow stromal cell-induced MM cell growth.
Kinase Assay	Recombinant enzymes in 20 mM Tris-HCl (pH 8.0), 2 mM CaCl2, and 2 mM β-mercaptoethanol are incubated with dose ranges of P005091 for 30 min in a 96-well plate before the addition of Ub-PLA2 and NBD C6-HPC or Ub-EKL and EKL substrate. The liberation of a fluorescent product within the linear range of the assay is monitored using a Perkin Elmer Envision fluorescence plate reader. Vehicle (2% [v/v] DMSO) and 10 mM N-ethylmaleimide (NEM) are included as controls.
Animal Research	Animal Models: CB-17 SCID-mice are subcutaneously inoculated with MM.1S, ARP-1, or RPMI-8226 cells in 100 μL of serum free RPMI-1640 medium. Formulation: P005091 is dissolved in 4% NMP(N-methyl-2-Pyrrolidone), 4% Tween-80, and 92% Milli-Q water at a final concentration of 2 mg/mL.
Synonyms	P5091

Chemical Properties

Molecular Weight	348.22
Formula	C₁₂H₇Cl₂NO₃S₂
Cas No.	882257-11-6
Smiles	CC(=O)c1cc(c(Sc2cccc(Cl)c2Cl)s1)[N+]([O-])=O
Relative Density.	1.60 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 68 mg/mL (195.28 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8717 mL	14.3587 mL	28.7175 mL	143.5874 mL
5 mM	0.5743 mL	2.8717 mL	5.7435 mL	28.7175 mL
10 mM	0.2872 mL	1.4359 mL	2.8717 mL	14.3587 mL
20 mM	0.1436 mL	0.7179 mL	1.4359 mL	7.1794 mL
50 mM	0.0574 mL	0.2872 mL	0.5743 mL	2.8717 mL
100 mM	0.0287 mL	0.1436 mL	0.2872 mL	1.4359 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc