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U7D-1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
U7D-1图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
U7D-1 是一种首创的、有效的和选择性的泛素特异性蛋白酶 7USP7 PROTAC降解剂，在 RS4;11 细胞中DC50为 33 nM。U7D-1 具有抗癌活性。U7D-1 可诱导 Jeko-1 细胞凋亡 (apoptosis)。
生物活性

U7D-1 is a first-in-class potent and selectiveUSP7(ubiquitin-specific protease 7)PROTACdegrader, with aDC50of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 inducesapoptosisin Jeko-1 cells[1].

IC50& Target

DC50: 33 nM (USP7 in RS4;11 cells)[1]

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.
分子量

940.14

Formula

C53H65N9O7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.