体外研究
(In Vitro) |
U7D-1 (0-1 μM, 0-24 h) induced USP7 degradation in RS4;11 cell, reducing the USP7 protein level by 83.2% at 1 μM[1].
U7D-1 (0-20 μM, 3 days) shows anti-proliferative activity in p53 wild-type cell lines, and maintains potent cell growth inhibition in p53 mutant cancer cells[1].
U7D-1 (1 μM, 0-24 h) upregulates the level of p53 and p21 proteins in a time-dependent manner, and induces cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner[1].
U7D-1 (1 μM, 24 h) up-regulates the expression of apoptotic related genes and down-regulates the expression of E2F related genes in Jeko-1 cells[1].
Western Blot Analysis[1]
| Cell Line: |
RS4;11 cells |
| Concentration: |
0, 5, 20, 50, 100, and 500 nM |
| Incubation Time: |
24 h |
| Result: |
Induced USP7 degradation in RS4;11 cell in a dose dependent manner, with a DC50(half-maximal degradation) value of 33 nM. |
Cell Proliferation Assay[1]
| Cell Line: |
p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines); p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM) |
| Concentration: |
0-20 μM |
| Incubation Time: |
3 days |
| Result: |
Showed antiproliferative activity in p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines), and p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM), with IC50values for 3 days of 79.4, 227.0, 830.3, 1367.2, 4948.0, 1034.9, 1175.3, 1860.6, 6077.6, 9078.0, and 10675.0, respectively. Had an antiproliferative activity with an IC50value of 53.5 nM in Jeko-1 cells for 7 days but exhibited a 13-fold loss in antiproliferative activity with an IC50value of 727 nM in Jeko-1 CRBN KO cells. |
Western Blot Analysis[1]
| Cell Line: |
RS4;11 cells, Jeko-1 and Mino cell |
| Concentration: |
1 μM |
| Incubation Time: |
0, 2, 4, 6, 8, 10, 12, 20, 24, 36, 48, 60, and 72 h |
| Result: |
USP7 degradation in RS4;11 cells induced by U7D-1 started after 4 h of exposure and more effective degradation was observed after 8 h of exposure. Up-regulated the level of p53 and p21 proteins in RS4;11 cells in a time-dependent manner. Had no effect on the level of p53 protein in p53-mutant cell lines. Induced cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner. |
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