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P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $32 | In Stock | |
5 mg | $52 | In Stock | |
10 mg | $83 | In Stock | |
25 mg | $167 | In Stock | |
50 mg | $319 | In Stock | |
100 mg | $476 | In Stock | |
1 mL x 10 mM (in DMSO) | $91 | In Stock |
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. |
Alias | P22077 |
Molecular Weight | 315.32 |
Formula | C12H7F2NO3S2 |
Cas No. | 1247819-59-5 |
Smiles | CC(=O)c1cc(c(Sc2ccc(F)cc2F)s1)[N+]([O-])=O |
Relative Density. | 1.53 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 31.5 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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