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P 22077

Catalog No. T2424   CAS 1247819-59-5
Synonyms: P22077

P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.

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P 22077 Chemical Structure
P 22077, CAS 1247819-59-5
Pack Size Availability Price/USD Quantity
2 mg In stock $ 32.00
5 mg In stock $ 52.00
10 mg In stock $ 83.00
25 mg In stock $ 167.00
50 mg In stock $ 319.00
100 mg In stock $ 476.00
1 mL * 10 mM (in DMSO) In stock $ 91.00
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Purity: 98.42%
Purity: 97.9%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.
Targets&IC50 USP7:8.6 μM(EC50)
In vivo P22077, administered at concentrations of 15-45 mM to cell lysates, inhibits a subset of DUBs (deubiquitinating enzymes) and prompts tumor cell death with an EC50 in the low micromolar range. Treatment with P22077 during the release from a G1/S arrest induced by hydroxyurea in U2OS cells results in a dose-dependent decrease in claspin protein levels, accompanied by reduced phosphorylation of serine 317 on Chk1. Furthermore, after P22077 exposure, quantitative mass spectrometry reveals diminished levels of E3 ubiquitin ligase components RBX1, DCAF7, DCAF11, and DNA damage-binding protein 1. While displaying negligible activity against DEN1 and SENP2 core, P22077 robustly inhibits USP7 with an IC50 of 8 μM, indicating selective inhibition towards USP7 and closely related DUB, USP47, over a range of DUBs, cysteine proteases, and other protease families in vitro.
Synonyms P22077
Molecular Weight 315.32
Formula C12H7F2NO3S2
CAS No. 1247819-59-5

Storage

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

Solubility Information

DMSO: 31.5 mg/mL (100 mM)

TargetMolReferences and Literature

1. Tian X, et al. Assay Drug Dev Technol, 2011, 9(2), 165-173. 2. Altun M, et al. Chem Biol, 2011, 18(11), 1401-1412. 3. Chen F, Zhang W, Xie D, et al. Histone chaperone FACT represses retrotransposon MERVL and MERVL-derived cryptic promoters[J. Nucleic Acids Research. 2020, 48(18): 10211-10225.

TargetMolCitations

1. Chen F, Zhang W, Xie D, et al. Histone chaperone FACT represses retrotransposon MERVL and MERVL-derived cryptic promoters. Nucleic Acids Research. 2020, 48(18): 10211-10225 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:
Inhibitor Library Anti-Cancer Compound Library Cell Cycle Compound Library DNA Damage & Repair Compound Library Autophagy Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Ubiquitination Compound Library HIF-1 Signaling Pathway Compound Library Anti-Aging Compound Library

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ML364 FT671 GNE-6776 USP28-IN-3 USP7-IN-5 KSQ-4279 IMP-1710 FT827

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Keywords

P 22077 1247819-59-5 Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Inhibitor P22077 P-22077 inhibit Deubiquitinase DUBs inhibitor

 

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