P5091
Based on 28 publication(s) in Google Scholar
P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
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- 純度: 99.90%
- CAS 番号: 882257-11-6
- 分子式: C12H7Cl2NO3S2
- 分子量:348.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Ubiquitination Compound Library
HY-L050
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Protease Inhibitor Library
HY-L147
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 P005091
More- Nat Commun. 2026 May 13;17(1):4331. [Abstract]
- Nat Commun. 2023 Feb 9;14(1):731. [Abstract]
- Metabolism. 2026 May:178:156553. [Abstract]
- Redox Biol. 2026 Jun 21:95:104271. [Abstract]
- Theranostics. 2022 May 16;12(9):4348-4373. [Abstract]
- J Exp Clin Cancer Res. 2019 Nov 15;38(1):468. [Abstract]
- Cell Death Dis. 2025 May 19;16(1):400. [Abstract]
- Cell Death Dis. 2024 Oct 15;15(10):749. [Abstract]
- Pharmacol Res. 2024 Jul:205:107235. [Abstract]
- Cell Death Dis. 2023 Dec 21;14(12):852. [Abstract]
- Cell Commun Signal. 2023 Nov 9;21(1):319. [Abstract]
- EBioMedicine. 2024 Feb:100:104961. [Abstract]
- J Transl Med. 2024 Dec 20;22(1):1135. [Abstract]
- Oncogene. 2022 Aug;41(33):4018-4027. [Abstract]
- EMBO J. 2022 Aug 16;41(16):e108791. [Abstract]
- Cell Rep. 2025 Nov 25;44(11):116476. [Abstract]
- Cell Rep. 2024 Oct 15;43(11):114872. [Abstract]
- Cell Rep. 2023 Apr 3;42(4):112339. [Abstract]
- J Med Chem. 2022 Oct 27;65(20):13645-13659. [Abstract]
- Cancer Gene Ther. 2026 Mar;33(3):277-288. [Abstract]
- FASEB J. 2021 Aug;35(8):e21800. [Abstract]
- Viruses. 2023 Feb 28;15(3):655. [Abstract]
- Mol Carcinog. 2019 Jan;58(1):42-54. [Abstract]
- Toxicon. 2026 Apr 1:273:109018. [Abstract]
- Neurol Res. 2024 Nov;46(11):1008-1017. [Abstract]
- bioRxiv. 2025 Aug 10.
- bioRxiv. 2025 July 04.
- SSRN. 2024 Feb 13.
Customer Validation & Images
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生物活性
EC50: 4.2 μM (USP7)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
11 μM
Compound: 1, P-005091
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Cytotoxicity against human HCT116 cells after 72 hrs
Cytotoxicity against human HCT116 cells after 72 hrs
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[PMID: 24900381] |
| Sf9 | IC50 |
4.2 μM
Compound: 1, P-005091
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Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay
Inhibition of recombinant USP7 expressed in Sf9 cells by Ub-CHOP reporter assay
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[PMID: 24900381] |
P005091 is a trisubstituted thiophene with dichlorophenylthio, nitro, and acetyl substituents mediating anti-USP7 activity. P005091 exhibits potent, specific, and selective deubiquitylating activity against USP7. In contrast, P005091 does not inhibit other DUBs or other families of cysteine proteases tested (EC50 > 100 mM). P005091 inhibits the labeling of USP7 with HA-UbVME in a concentration-dependent manner. USP7-mediated cleavage of high molecular weight polyubiquitin chains is inhibited in a dose-dependent manner by P005091. Moreover, P005091 inhibits USP7- but not USP2- or USP8-mediated cleavage of poly K48-linked ubiquitin chains. USP7 inhibition by P005091 induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P005091 inhibits USP7 deubiquitylating activity, without blocking proteasome activity in MM Cells. P005091 inhibits growth in MM cells and overcomes bortezomib-resistance. P005091 induces a dose-dependent decrease in viability of various MM cell lines, including those that are resistant to conventional therapies dexamethasone (Dex) (MM.1R), doxorubicin (Dox-40), or melphalan (LR5) (IC50 range 6-14 μM). P005091 overcomes bone marrow stromal cell-induced growth of MM Cells. P005091 decreases HDM2 and HDMX, as well as upregulated p53 and p21 levels. Overall, P005091-induced cytotoxicity is mediated in part via HDM2-p21 signaling axis and although p53 is upregulated in response to P005091 treatment, the cytotoxic activity of P005091 is not dependent on p53[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 882257-11-6
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性状 Solid
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分子量 348.22
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分子式 C12H7Cl2NO3S2
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Color Light yellow to yellow
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SMILES
CC(C1=CC([N+]([O-])=O)=C(SC2=CC=CC(Cl)=C2Cl)S1)=O
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別名
P005091
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (28)
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Journal Impact Factor
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Most Recent
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Nat Commun
Targeted degradation of USP7 in solid cancer cells reveals distinct effects of deubiquitinase degraders and inhibitors. [Abstract]2026 May 13;17(1):4331. PMID: 42129197 -
Nat Commun
Angiotensin-converting enzyme inhibitor promotes angiogenesis through Sp1/Sp3-mediated inhibition of notch signaling in male mice. [Abstract]2023 Feb 9;14(1):731. PMID: 36759621 -
Metabolism
PFKFB3 nuclear translocation improves diabetic retinopathy by attenuating endothelial cell senescence through inhibition of USP7-p53 axis. [Abstract]2026 May:178:156553. PMID: 41655956 -
Redox Biol
S100A9 modulates USP7-mediated stabilization of NCOA4 to promote ferroptosis in sepsis-associated acute lung injury. [Abstract]2026 Jun 21:95:104271. PMID: 42330601 -
Theranostics
RNA interference screens discover proteases as synthetic lethal partners of PI3K inhibition in breast cancer cells. [Abstract]2022 May 16;12(9):4348-4373. PMID: 35673573 -
J Exp Clin Cancer Res
USP7 is a novel Deubiquitinase sustaining PLK1 protein stability and regulating chromosome alignment in mitosis. [Abstract]2019 Nov 15;38(1):468. PMID: 31730000
P005091 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Nov 15;38(1):468. [Abstract]
DU145 and VCaP cells are treated with the USP7 inhibitor P5091 for 24 h, and the protein levels of USP7 and PLK1 are assessed by immunoblotting.
P005091 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Nov 15;38(1):468. [Abstract]
DU145 and VCaP cells are treated with the USP7 inhibitor P5091 for 24 h, and the protein levels of USP7 and PLK1 are assessed by immunoblotting.
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Cell Death Dis
Synergistic regulation of DACH1 stability by acetylation and deubiquitination promotes colorectal cancer progression. [Abstract]2025 May 19;16(1):400. PMID: 40389405 -
Cell Death Dis
USP7 depletion potentiates HIF2α degradation and inhibits clear cell renal cell carcinoma progression. [Abstract]2024 Oct 15;15(10):749. PMID: 39406703 -
Pharmacol Res
USP7 promotes cardiometabolic disorders and mitochondrial homeostasis dysfunction in diabetic mice via stabilizing PGC1β. [Abstract]2024 Jul:205:107235. PMID: 38815879 -
Cell Death Dis
USP7 inhibits the progression of nasopharyngeal carcinoma via promoting SPLUNC1-mediated M1 macrophage polarization through TRIM24. [Abstract]2023 Dec 21;14(12):852. PMID: 38129408 -
Cell Commun Signal
Inhibition of USP7 upregulates USP22 and activates its downstream cancer-related signaling pathways in human cancer cells. [Abstract]2023 Nov 9;21(1):319. PMID: 37946202 -
EBioMedicine
CRIP1 involves the pathogenesis of multiple myeloma via dual-regulation of proteasome and autophagy. [Abstract]2024 Feb:100:104961. PMID: 38199044 -
J Transl Med
Ubiquitin-specific protease 7 maintains c-Myc stability to support pancreatic cancer glycolysis and tumor growth. [Abstract]2024 Dec 20;22(1):1135. PMID: 39707401 -
Oncogene
2022 Aug;41(33):4018-4027. PMID: 35821281 -
EMBO J
USP8 promotes cancer progression and extracellular vesicle-mediated CD8+ T cell exhaustion by deubiquitinating the TGF-β receptor TβRII. [Abstract]2022 Aug 16;41(16):e108791. PMID: 35811497 -
Cell Rep
IGF2BP2 stabilized by USP7 promotes cancer-associated fibroblast activation and attenuates gemcitabine sensitivity in PDAC. [Abstract]2025 Nov 25;44(11):116476. PMID: 41201091 -
Cell Rep
2024 Oct 15;43(11):114872. PMID: 39412987 -
Cell Rep
2023 Apr 3;42(4):112339. PMID: 37014752 -
J Med Chem
Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer. [Abstract]2022 Oct 27;65(20):13645-13659. PMID: 36221183 -
Cancer Gene Ther
WTAP stabilized by USP7 contributes to enzalutamide resistance in prostate cancer via mediating AKT m6A-modification. [Abstract]2026 Mar;33(3):277-288. PMID: 41981278 -
FASEB J
2021 Aug;35(8):e21800. PMID: 34324733 -
Viruses
Inhibitors of the Ubiquitin-Mediated Signaling Pathway Exhibit Broad-Spectrum Antiviral Activities against New World Alphaviruses. [Abstract]2023 Feb 28;15(3):655. PMID: 36992362 -
Mol Carcinog
Targeting the overexpressed USP7 inhibits esophageal squamous cell carcinoma cell growth by inducing NOXA-mediated apoptosis. [Abstract]2019 Jan;58(1):42-54. PMID: 30182448
P005091 purchased from MedChemExpress. Usage Cited in: Mol Carcinog. 2019 Jan;58(1):42-54. [Abstract]
Treatment with P5091 increases the cleavage of CASP9, CASP3, and PARP. ESCC cells Kyse450, Kyse510 and Kyse30 are treated with P5091 for 72 h and cell lysates are assessed by western blotting with specific antibodies against cleaved CASP9, CASP3, or PARP. GAPDH is used as a control.
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Toxicon
Toosendanin sensitizes hepatocyte ferroptosis via dual inhibition of Nrf2 O-GlcNAcylation and USP7-driven deubiquitination. [Abstract]2026 Apr 1:273:109018. PMID: 41628670 -
Neurol Res
USP7 alleviates neuronal inflammation and apoptosis in spinal cord injury via deubiquitinating NRF1/KLF7 axis. [Abstract]2024 Nov;46(11):1008-1017. PMID: 39007840 -
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溶剤 & 溶解度
DMSO : 25 mg/mL (71.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
For the animal study, 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. The human plasmacytoma xenograft model is performed as previously described. 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. When tumors are measurable (100-180 mm3), mice are randomized into treatment groups. In the SCID-hu model, human fetal bone grafts are subcutaneously implanted into SCID mice. Four weeks after bone implantation, INA-6 cells are injected directly into the fetal bone implant in SCID mice; and as a measure of tumor burden, mouse sera samples are analyzed for shIL-6R by ELISA. Upon detection of shIL-6R, mice are treated with vehicle or P005091, and mouse serum is analyzed for alterations in shIL-6R levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8717 mL | 14.3587 mL | 28.7175 mL | 71.7937 mL |
| 5 mM | 0.5743 mL | 2.8717 mL | 5.7435 mL | 14.3587 mL | |
| 10 mM | 0.2872 mL | 1.4359 mL | 2.8717 mL | 7.1794 mL | |
| 15 mM | 0.1914 mL | 0.9572 mL | 1.9145 mL | 4.7862 mL | |
| 20 mM | 0.1436 mL | 0.7179 mL | 1.4359 mL | 3.5897 mL | |
| 25 mM | 0.1149 mL | 0.5743 mL | 1.1487 mL | 2.8717 mL | |
| 30 mM | 0.0957 mL | 0.4786 mL | 0.9572 mL | 2.3931 mL | |
| 40 mM | 0.0718 mL | 0.3590 mL | 0.7179 mL | 1.7948 mL | |
| 50 mM | 0.0574 mL | 0.2872 mL | 0.5743 mL | 1.4359 mL | |
| 60 mM | 0.0479 mL | 0.2393 mL | 0.4786 mL | 1.1966 mL |
P005091 関連分類
HY-15667 関連分類
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