Cas No.: | 1247819-59-5 |
Chemical Name: | P 22077; P-22077 |
Synonyms: | P 22077; P-22077 |
SMILES: | CC(=O)C1=CC(=C(S1)SC2=C(C=C(C=C2)F)F)[N+](=O)[O-] |
Formula: | C12H7F2NO3S2 |
M.Wt: | 315.32 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. It also inhibits USP47 with an EC50 of 8.74 μM. |
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]. |
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]. |