PARP1/BRD4-IN-1 是一种有效、且具有高选择性的PARP1/BRD4抑制剂，PARP1 与 BRD4 的 IC50分别为 49 nM 与 202 nM。PARP1/BRD4-IN-1 通过抑制 PARP1 和 BRD4 的表达与活性，协同抑制胰腺癌细胞的恶性生长。
| 生物活性 | PARP1/BRD4-IN-1 is a potent and high selectivePARP1/BRD4inhibitor (IC50s of 49 and 202 nM inPARP1andBRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity ofPARP1andBRD4to synergistically inhibit the malignant growth of pancreaticcancercells[1]. |
| IC50& Target | BRD4 202 nM (IC50) | PARP1 49 nM (IC50) |
|
体外研究
(In Vitro) | PARP1/BRD4-IN-1 (compound III-7) (0-2 μM; 3-7 days) has potent inhibition of the growth of cancer cell lines[1].
PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) can significantly inhibit the expression of PARP1 and BRD4 at 2 μM in SW1990 cells[1].
PARP1/BRD4-IN-1 (1, 2 μM; 4 days) arrests the cell cycle at G0/G1and G2/M phase in SW1990 cells[1].
PARP1/BRD4-IN-1 (0, 1, 2 μM; 4 days) has the potent efficacy on the apoptosis of SW1990 cells at 2 μM[1].
PARP1/BRD4-IN-1 (1, 2 μM; 4 days) regulates the expression of HEXIM1, c-Myc, FOXO1, MDC1 and TOPBP1 to enhance the inhibition of DNA repair in SW1990 cells[1].
Cell Proliferation Assay | Cell Line: | CFPAC-1, SW1990, MDA-MB-231, MDA-MB-468, HCT-116, THP-1[1] | | Concentration: | 0-2 μM | | Incubation Time: | 3, 4 or 7 days | | Result: | Showed potent inhibition of the growth of cancer cell lines. |
Western Blot Analysis | Cell Line: | SW1990[1] | | Concentration: | 0, 1, 2 μM | | Incubation Time: | 4 days | | Result: | Significantly inhibited the expression of PARP1 and BRD4 at 2 μM. |
Cell Cycle Analysis | Cell Line: | SW1990[1] | | Concentration: | 1, 2 μM | | Incubation Time: | 4 days | | Result: | Arrested the cell cycle at G0/G1and G2/M phase. |
Apoptosis Analysis | Cell Line: | SW1990[1] | | Concentration: | 0, 1, 2 μM | | Incubation Time: | 4 days | | Result: | Showed potent efficacy on the apoptosis of SW1990 cells at 2 μM. |
|
体内研究
(In Vivo) | PARP1/BRD4-IN-1 (30mg/kg; intraperitoneal injection for 28 days) can significantly inhibit the tumor size and weight, and does not cause significant damage of the kidney, lung, spleen, liver and heart in mice[1].
| Animal Model: | Athymic nude mice (6-7 weeks, 18-20 g, SW1990-injected)[1] | | Dosage: | 30mg/kg | | Administration: | Intraperitoneal injection for 28 days | | Result: | Significantly inhibited the tumor size and weight and did not cause significant damage of the kidney, lung, spleen, liver and heart. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 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. |
