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P005091

Catalog No. T6925 CAS 882257-11-6

Synonyms: P5091

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

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P005091, CAS 882257-11-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 158.00
50 mg	In stock	$ 270.00
100 mg	In stock	$ 432.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 99.87%

Purity: 99.82%

Purity: 99.53%

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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
Molecular Weight	348.22
Formula	C12H7Cl2NO3S2
CAS No.	882257-11-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 68 mg/mL, Sonification is recommended.

References and Literature

1. Chauhan D, et al. Cancer Cell, 2012, 22(3), 345-358. 2. Weinstock J, et al. ACS Med Chem Lett. 2012, 3(10):789-92. 3. Park, Su H., et al. Posttranslational regulation of FOXA1 by Polycomb and BUB3/USP7 deubiquitin complex in prostate cancer. Science Advances. 7.15 (2021): eabe2261.

Citations

1. Park, Su H., et al. Posttranslational regulation of FOXA1 by Polycomb and BUB3/USP7 deubiquitin complex in prostate cancer.. Science Advances. 2021 Apr 7;7(15):eabe2261. doi: 10.1126/sciadv.abe2261. Print 2021 Apr. 2. Wu W, Xu H, Liao C, et al. Blockade of USP14 potentiates type I interferon signaling and radiation-induced antitumor immunity via preventing IRF3 deubiquitination. Cellular Oncology. 2022: 1-15 3. Yue X, Liu T, Wang X, et al.Pharmacological inhibition of BAP1 recruits HERC2 to competitively dissociate BRCA1–BARD1, suppresses DNA repair and sensitizes CRC to radiotherapy.Acta Pharmaceutica Sinica B.2023

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Aging Compound Library Anti-Cancer Compound Library Hematonosis Compound Library Protease Inhibitor Library HIF-1 Signaling Pathway Compound Library Bioactive Compound Library DNA Damage & Repair Compound Library Ubiquitination Compound Library

Related Products

Related compounds with same targets

USP7-IN-1 USP28-IN-3 GNE-6776 BAY 11-7082 USP30 inhibitor 11 B-AP15 Spautin-1 HBX 41108

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Keywords

P005091 882257-11-6 Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB inhibit P 5091 Deubiquitinase P-5091 P5091 P 005091 DUBs Inhibitor P-005091 inhibitor

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