P5091

SKU: orb1300341

Description

P005091 is a potent and selective small molecule inhibitor of the deubiquitinase USP7, exhibiting an EC50 of 4.2 µM. It is widely used in biochemical and cellular research to study the role of USP7 in pathways such as p53 regulation, epigenetics, and oncology, facilitating both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 882257-11-6
• MW: 348.23
• Purity: >98%
• Formula: C₁₂H₇Cl₂NO₃S₂
• SMILES: CC(=O)c1cc(c(Sc2cccc(Cl)c2Cl)s1)[N+]([O-])=O
• Target: DUB (Deubiquitinating enzyme)
• Solubility: Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 40 mg/ml with warming).

Bioactivity

• Target IC50:
  USP7:4.2 μM
• 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.
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• 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.
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• 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.
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

P005091, P-005091, P 5091, P 005091, USP7, Inhibitor, P5091, P-5091, inhibit, DUBs, Deubiquitinase

Compound Identifiers

PubChem CID

2819993