P5091 --- Ubiquitin-specific Protease 7 (USP7) Inhibitor

P5091 (P005091) is a novel potent and selective inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 ~4.2 μM. It does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). It induces apoptosis in MM cells resistant to conventional and bortezomib therapies. Biochemical and genetic studies showed that blockade of HDM2 and p21 abrogated P5091-induced cytotoxicity. In animal tumor model studies, P5091 was well tolerated, and it inhibited tumor growth, and prolongs survival. Combining P5091 with lenalidomide, HDAC inhibitor SAHA, or dexamethasone triggered synergistic anti-MM activity.

Product information

CAS Number: 882257-11-6

Molecular Weight: 348.22

Formula: C12H7Cl2NO3S2

Synonym:

P005091

Chemical Name: 1-(5-((2,3-dichlorophenyl)thio)-4-nitrothiophen-2-yl)ethanone

Smiles: CC(=O)C1=CC(=C(S1)SC1=CC=CC(Cl)=C1Cl)[N+]([O-])=O

InChiKey: LKZLGMAAKNEGCH-UHFFFAOYSA-N

InChi: InChI=1S/C12H7Cl2NO3S2/c1-6(16)10-5-8(15(17)18)12(20-10)19-9-4-2-3-7(13)11(9)14/h2-5H,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

P5091 was used at 5-12.5 µM final concentration in various in vitro assays.

In Vivo:

P5091 was administered through IV injection at 10 mg/kg twice weekly for 3 weeks.

References:

1. Chauhan D, et al. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. (2012) Cancer Cell. 22(3):345-58.

Products are for research use only. Not for human use.

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