Art. -Nr.: HY-13865

P 22077

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC₅₀ of 8.01 μM. P 22077 also inhibits USP47 with an EC₅₀ of 8.74 μM.

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Reinheit: 98.42%
CAS. Nr.: 1247819-59-5
Formel: C₁₂H₇F₂NO₃S₂
Molecular Weight:315.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

P 22077 Chemical Structure

CAS. Nr.: 1247819-59-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC₅₀ of 8.01 μM. P 22077 also inhibits USP47 with an EC₅₀ of 8.74 μM.

IC₅₀ & Target

EC50: 8.01 μM (USP7), 8.74 μM (USP47)^[1]

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	8.82 μM Compound: P22077	Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells expressing wild type p53 assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28108249]
Sf9	IC₅₀	8 μM Compound: 4	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	[PMID: 24900381]

In Vitro

P 22077 is an inhibitor of USP7 and DUB USP47, with EC₅₀s of 8.01 μM and 8.74 μM, respectively. P 22077 (15-45 μM) inhibits a much smaller subset of DUBs. P 22077 (25 μM) causes DUBs inhibition in HEK293T cells^[1]. P 22077 (0-20 μM) greatly reduces the cell viability of Neuroblastoma (NB) cells including IMR-32, NGP, CHLA-255, and SH-SY5Y cells but without NB-19 and SK-N-AS cells. P 22077 (10 μM) increases p53 activity and induces apoptosis in p53 wild-type and HDM2-expressing NB cells. P 22077 (5 μM) enhances the cytotoxic effect of Dox and VP-16 on NB cells, and enhances Dox- and VP-16-induced p53-mediated apoptosis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

P 22077 (15 mg/kg, i.p. 21 days) shows potent antitumor activities in an xenograft mouse model bearing IMR-32-derived tumors; P 22077 also exhibits antitumor effects after treatment at 10 mg/kg for 14 days in mice bearing SH-SY5Y-derived tumors, and at 20 mg/kg for 12 days in mice bearing NGP-derived tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1247819-59-5
Appearance Solid
Molecular Weight 315.32
Formel C₁₂H₇F₂NO₃S₂
Color Light yellow to yellow
SMILES

CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (24)

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Journal Impact Factor

Nat Commun

USP2 inhibition unleashes CD47-restrained phagocytosis and enhances anti-tumor immunity. [Abstract]

2025 May 16;16(1):4564. PMID: 40379682
Nat Commun

The adaptor protein AP-3β disassembles heat-induced stress granules via 19S regulatory particle in Arabidopsis. [Abstract]

2025 Feb 27;16(1):2039. PMID: 40016204
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
Nat Commun

USP8 inhibition reshapes an inflamed tumor microenvironment that potentiates the immunotherapy. [Abstract]

2022 Mar 31;13(1):1700. PMID: 35361799
Nat Chem Biol

Inhibition of USP10 induces degradation of oncogenic FLT3. [Abstract]

2017 Dec;13(12):1207-1215. PMID: 28967922

P 22077 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2017 Dec;13(12):1207-1215. [Abstract]

The effects of HBX19818 on FLT 3 expression in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment. The effects of P22077 on FLT 3 levels in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment.
J Immunother Cancer

CD47 destabilization via manipulating the SPOP-USP2 axis augments macrophage phagocytosis and cancer immunotherapy. [Abstract]

2026 Jan 14;14(1):e013498. PMID: 41534899
Cell Death Dis

SPOP and HAUSP bidirectionally regulate LZTS2 ubiquitination to modulate the Wnt pathway. [Abstract]

2025 Dec 24. PMID: 41436424
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
Cell Death Dis

USP7 regulates the ERK1/2 signaling pathway through deubiquitinating Raf-1 in lung adenocarcinoma. [Abstract]

2022 Aug 10;13(8):698. PMID: 35948545
Haematologica

Deubiquitylase USP7 regulates human terminal erythroid differentiation by stabilizing GATA1. [Abstract]

2019 Nov;104(11):2178-2187. PMID: 30872372
Biomed Pharmacother

Suppression of USP7 negatively regulates the stability of ETS proto-oncogene 2 protein. [Abstract]

2023 Jun:162:114700. PMID: 37062218
Oncogene

Helicobacter pylori activates DOPEY1 to promote p53 degradation through the USP7/TRIP12 axis in gastric tumorigenesis. [Abstract]

2025 May;44(18):1245-1258. PMID: 39939725
PLoS Biol

USP7 facilitates brain tumor survival upon glucose deprivation by regulating phosphofructokinase muscle-type nuclear translocation in mice. [Abstract]

2026 Mar 12;24(3):e3003698. PMID: 41818193
Cell Chem Biol

Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2. [Abstract]

2021 Jun 17;28(6):855-865.e9. PMID: 33979649
Cell Death Discov

USP7 promotes endothelial activation to aggravate sepsis-induced acute lung injury through PDK1/AKT/NF-κB signaling pathway. [Abstract]

2025 Apr 17;11(1):183. PMID: 40246841
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
Br J Cancer

Inhibition of the deubiquitinase USP10 induces degradation of SYK. [Abstract]

2020 Apr;122(8):1175-1184. PMID: 32015510
J Mol Biol

Cellular assays for dynamic quantification of deubiquitinase activity and inhibition. [Abstract]

2023 Dec 1;435(23):168316. PMID: 37858708
Mol Neurobiol

LncRNA ZNF883-Mediated NLRP3 Inflammasome Activation and Epilepsy Development Involve USP47 Upregulation. [Abstract]

2022 Aug;59(8):5207-5221. PMID: 35678979
Med Oncol

Tetrahydrobiopterin induces proteasome inhibitor resistance and tumor progression in multiple myeloma. [Abstract]

2022 Feb 12;39(5):55. PMID: 35150316
Toxicol Appl Pharmacol

Artesunate attenuates osteoarthritis in mice by promoting MTA1 transcription through a USP7/FoxO1 axis. [Abstract]

2024 Aug 20:117075. PMID: 39173720
Anim Cells Syst

Blocking SLC7A11 attenuates the proliferation of esophageal squamous cell carcinoma cells. [Abstract]

2024 May 11;28(1):237-250. PMID: 38741950
J Leukoc Biol

S100A9 promotes inflammasome-dependent autoinflammation by blocking the degradation of SYK tyrosine kinase. [Abstract]

2025 Sep 1;117(9):qiaf129. PMID: 40966542
J Oncol

Trained Immunity of IL-12-, IL-15-, and IL-18-Induced CD3+CD56+ NKT-Like Cells. [Abstract]

2022 Jun 23;2022:8724933. PMID: 35783158

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (158.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1714 mL

15.8569 mL

31.7138 mL

5 mM

0.6343 mL

3.1714 mL

6.3428 mL

10 mM

0.3171 mL

1.5857 mL

3.1714 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 5 mg/mL (15.86 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Recombinant full length USP7, USP2 core, USP5, JOSD2, DEN1, PLpro core, and SENP2 catalytic core are generated. Amino terminal His6 tagged USP4, USP8, USP28, UCH-L1, UCH-L3, UCH-L5, and MMP13 are expressed in Escherichia coli. N-terminal His6 tagged USP15, USP20, and USP47 are expressed in Sf9 cells. All the recombinant proteins are purified by chromatography. Amino terminal tagged His6 Ub-PLA2 (Ub-CHOP), SUMO3-PLA2 (SUMO3-CHOP), ISG15-PLA2 (ISG15-CHOP), NEDD8-PLA2 (NEDD8-CHOP), Ub-EKL (Ub-CHOP2), and free catalytically active PLA2 are prepared^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

Cell viability assays are assessed using the Cell Counting Kit-8 (CCK-8, WST-8[2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2 H-tetrazolium, monosodium salt]). Cells are seeded in 96-well flat-bottomed plates at the density of 1 × 10⁴ per well. After 24 h of incubation at 37°C, increasing concentrations of P 22077, Dox, VP-16, or their combinations are added to the wells. Twenty-four hours later, 10 μL of CCK-8 is added into each well and after 1 h of incubation, the absorbance is measure at 450 nm using the microplate reader. Each experiment is performed in replicates of six. Background reading of media only is used to normalize the results^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

The orthotopic Neuroblastoma (NB) mouse model is used in the assay. Briefly, 1.5 × 10⁶ human IMR-32, SH-SY5Y, or NGP cells with luciferase expression are surgically injected into the left renal capsule of 5-week-old female NCR nude mice. IMR-32, SH-SY5Y, and NGP-derived xenografts are allowed to grow for ~2-3 weeks before randomizing the mice into a control group and a P 22077 treatment group. Each group consists of three or six mice. Animals are treated with DMSO or P 22077 by intraperitoneal (i.p.) injection every day for 12, 14, or 21 days. At the end of the experiments, all mice are killed. Tumors and the right side control kidneys are resected, weighed, and photographed^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (596 KB)
- English - EN (596 KB)
- Français - FR (596 KB)
- Deutsch - DE (596 KB)
- Norwegian - NO (596 KB)
- Español - ES (596 KB)
- Swedish - SV (596 KB)
- Italian - IT (596 KB)
- Portuguese - PT (596 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Altun M, et al. Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem Biol. 2011 Nov 23;18(11):1401-12. [Content Brief]

[2]. Fan YH, et al. USP7 inhibitor P22077 inhibits neuroblastoma growth via inducing p53-mediated apoptosis. Cell Death Dis. 2013 Oct 17;4:e867. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.1714 mL	15.8569 mL	31.7138 mL	79.2845 mL
	5 mM	0.6343 mL	3.1714 mL	6.3428 mL	15.8569 mL
	10 mM	0.3171 mL	1.5857 mL	3.1714 mL	7.9285 mL
	15 mM	0.2114 mL	1.0571 mL	2.1143 mL	5.2856 mL
	20 mM	0.1586 mL	0.7928 mL	1.5857 mL	3.9642 mL
	25 mM	0.1269 mL	0.6343 mL	1.2686 mL	3.1714 mL
	30 mM	0.1057 mL	0.5286 mL	1.0571 mL	2.6428 mL
	40 mM	0.0793 mL	0.3964 mL	0.7928 mL	1.9821 mL
	50 mM	0.0634 mL	0.3171 mL	0.6343 mL	1.5857 mL
	60 mM	0.0529 mL	0.2643 mL	0.5286 mL	1.3214 mL
	80 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9911 mL
	100 mM	0.0317 mL	0.1586 mL	0.3171 mL	0.7928 mL

Keywords

P 22077

24 Cited Publications

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P 22077

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) P 22077

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

P 22077

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Ubiquitination Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) P 22077

Alle Deubiquitinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

P 22077 Related Classifications

Art. -Nr.: HY-13865