Molecular Formula | C12H7F2NO3S2 |
Molar Mass | 315.32 |
Density | 1.53±0.1 g/cm3(Predicted) |
Melting Point | 146 - 148°C |
Boling Point | 395.4±42.0 °C(Predicted) |
Solubility | Soluble in DMSO (up to 25 mg/ml) |
Appearance | solid |
Color | Off-white |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | P22077 is a recently discovered analog of the USP7 inhibitor p5091. P22077 had little activity on DEN1 and SENP2core over the range of concentrations tested, but inhibited USP7 with an IC50 of 8 μm. In vitro, P22077 inhibits a group of DUBs, cysteine proteases, and other family proteolytic enzymes, suggesting that P22077 inhibits USP7 and its closely related DUB usp47. 15-45 mM P22077 acts on the cell lysate to inhibit a small portion of the DUBs. P22077 induces tumor cell death with an EC50 in the low micromolar range. Unlike a wide range of specific inhibitors, the inhibitory effect of P22077 is altered at the ubiquitinated protein level. Treatment of U2OS cells in G1/S phase with P22077 induced the production of hydroxyurea, which resulted in a dose-dependent reduction of classin protein, with a consequent reduction in phosphoserine 317 chk1. Furthermore, after P22077 treatment of cells, quantitative MS demonstrated a reduction in the E3 ubiquitin ligase fractions RBX1, DCAF7, DCAF11, and DNA damage binding protein 1(DDB1). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.171 ml | 15.857 ml | 31.714 ml |
5 mM | 0.634 ml | 3.171 ml | 6.343 ml |
10 mM | 0.317 ml | 1.586 ml | 3.171 ml |
5 mM | 0.063 ml | 0.317 ml | 0.634 ml |
biological activity | P22077 is a ubiquitin-specific protease USP7 (ubiquitin-specific protease USP7) inhibitor, EC50 is 8.6 μM, which also inhibits USP47. |
In vitro studies | P22077 is an analog of the recently discovered USP7 inhibitor P5091. In the experimental concentration range, P22077 has little activity on DEN1 and SENP2core, but inhibits USP7 with IC50 of 8 μM. In vitro, P22077 inhibits a group of DUBs, cysteine proteases, and other family proteolytic enzymes, indicating that P22077 inhibits USP7 and its closely related DUB USP47. 15-45 mM P22077 acts on cell lysate and inhibits a small part of DUBs. P22077 induces tumor cell death, and EC50 is a low micromolar range. Unlike a wide range of specific inhibitors, the inhibitory effect of P22077 at the ubiquitinated protein level is altered. P22077 treated U2OS cells in G1/S phase induced the production of hydroxyurea, resulting in a decrease in Claspin protein. This effect is dose-dependent, with a decrease in phosphate serine 317 Chk1. Moreover, after P22077 treatment of cells, quantitative MS indicated that E3 ubiquitin ligase components RBX1, DCAF7, DCAF11, and DNA damage binding protein 1(DDB1) decreased. |