BRD4 Inhibitor-25 是一种BRD4抑制剂，对 BRD4 的 BD1 和 BD2 结构域的IC50为 0.82 μM，1.94 μM。BRD4 Inhibitor-25 在卵巢癌细胞中诱导凋亡和自噬细胞死亡。 BRD4 Inhibitor-25 可用于癌症、心血管、神经肌肉和炎症性疾病的研究。
| 生物活性 | BRD4Inhibitor-25 is aBRD4inhibitor withIC50s of 0.82 μM, 1.94 μM forBD1andBD2domains ofBRD4.BRD4Inhibitor-25 induces apoptotic andautophagycell death in ovariancancercells.BRD4Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders. |
| IC50& Target[1] | BRD4-BD1 0.82 μM (IC50) | BRD4 (BD2) 1.94 μM (IC50) | BRD4 BD1 0.419 μM (Ki) | BRD4 BD2 0.686 μM (Ki) | BRD2 BD1 15.91 μM (IC50) | BRD2 BD1 7.43 μM (Ki) |
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体外研究
(In Vitro) | BRD4 Inhibitor-25 (化合物 11a) 抑制 OC 细胞系 (SKOV-3、OVCAR-3、SW626、ES-2 和 A2780) 的细胞增殖[1]。
BRD4 Inhibitor-25 (当用过量的半胱氨酸处理时) 促进中等水平的 NO 释放 (10.587 μM)[1]。
BRD4 Inhibitor-25 (1 和 2 μM，24 小时) 诱导 SKOV-3 细胞凋亡和自噬[1]。
BRD4 Inhibitor-25 (2 μM，24 小时) 抑制自噬体和溶酶体融合，从而阻断 SKOV-3 细胞中的自噬通量[1]。
Cell Viability Assay[1] | Cell Line: | OC cell lines (SKOV-3, OVCAR-3, SW626, ES-2 and A2780) | | Concentration: | 0-20 μM approximately | | Incubation Time: | 24 h | | Result: | Inhibited cell proliferation with IC50s of 1.38, 2.69, 8.47, 3.44, 3.44 μM respectively. |
Western Blot Analysis[1] | Cell Line: | SKOV-3 cells | | Concentration: | 2 μM | | Incubation Time: | 24 h | | Result: | Increased cytochrome c and cleaved-caspase 3.
Reduced the anti-apoptosis protein Bcl-2.
Increased the autophagy-related proteins LC3II/I, p62/SQSTM1, and Beclin1. |
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体内研究
(In Vivo) | BRD4 Inhibitor-25 (化合物 11a，30 mg/kg，腹腔注射) 抑制 SKOV-3 皮下异种移植模型中的肿瘤生长[1]。
| Animal Model: | SKOV-3 subcutaneous xenograft model[1] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Reduced Ki-67, a cell proliferation marker (IHC staining). |
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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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