PROTAC BRD4 Degrader-6 (compound 32a) 是一种有效的小分子BRD4降解剂, BRD4 BD1 的IC50值为 2.7 nM。PROTAC BRD4 Degrader-6 能有效降解 BRD4 蛋白并抑制 c-Myc 的表达。PROTAC BRD4 Degrader-6 能抑制胰腺癌细胞系 BxPC3 的增殖并诱导细胞凋亡。PROTAC BRD4 Degrader-6 可用于人类胰腺癌研究。
| 生物活性 | PROTACBRD4 Degrader-6 (compound 32a) is a potent small-moleculeBRD4degrader withIC50value of 2.7 nM forBRD4BD1.PROTACBRD4 Degrader-6 potently degradesBRD4protein and inhibits the expression ofc-Myc.PROTACBRD4 Degrader-6 inhibits the proliferation of pancreaticcancercell line BxPC3 and inducesapoptosis.PROTACBRD4 Degrader-6 can be used for human pancreaticcancerresearch[1]. |
| IC50& Target[1] | BRD4 BD1 2.7 μM (IC50) | Caspase 3 |
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体外研究
(In Vitro) | PROTAC BRD4 Degrader-6 (compound 32a) (72 hours; BxPC3 cell) has anti-proliferation activity with IC50value of 0.165 μM[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces BRD4 protein degradation in a time-dependent manner, which results in the continuous decrease of c-Myc expression[1].
PROTAC BRD4 Degrader-6 (compound 32a) (1 μM; 48 hours; BxPC3 cell) induces the cell cycle arrest and apoptosis[1].
Western Blot Analysis[1] | Cell Line: | BxPC3 cell | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | Degraded BRD4 protein in a time-dependent manner and inhibits the expression of c-Myc. |
Cell Cycle Analysis[1] | Cell Line: | BxPC3 cell | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | Increase in G0/G1 and G2/M phase cells, and a decrease of S phase cells. |
Apoptosis Analysis[1] | Cell Line: | BxPC3 cell | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | The percentage of cells in early and late apoptosis was recorded as 10.10% and 12.36%, respectively. |
Western Blot Analysis[1] | Cell Line: | BxPC3 cell | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | The expression of caspase 3 and cleaved-caspase 3 significantly increased. |
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| 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. |
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