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PBRM1-BD2-IN-5 是一种有效的 PBRM1 Bromodomain 抑制剂,对 PBRM1-BD2 和 PBRM1-BD5 的 Kd 分别为 1.5 μM 和 3.9 μM,对 PBRM1-BD2 的 IC50 为 0.26 μM。PBRM1-BD2-IN-5 减少细胞裂解物中 PBAF 复合体全长 PBRM1 与乙酰化组蛋白肽的结合。PBRM1-BD2-IN-5 可用于抗癌研究。
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PBRM1-BD2-IN-5 是一种有效的 PBRM1 Bromodomain 抑制剂,对 PBRM1-BD2 和 PBRM1-BD5 的 Kd 分别为 1.5 μM 和 3.9 μM,对 PBRM1-BD2 的 IC50 为 0.26 μM。PBRM1-BD2-IN-5 减少细胞裂解物中 PBAF 复合体全长 PBRM1 与乙酰化组蛋白肽的结合。PBRM1-BD2-IN-5 可用于抗癌研究。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 696 | 现货 | |
2 mg | ¥ 948 | 现货 | |
5 mg | ¥ 1,420 | 现货 | |
10 mg | ¥ 2,110 | 现货 | |
25 mg | ¥ 3,370 | 现货 | |
50 mg | ¥ 4,470 | 现货 | |
100 mg | ¥ 5,910 | 现货 | |
500 mg | ¥ 11,800 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,300 | 现货 |
产品描述 | PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, demonstrating dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and boasts an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between the full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, which positions it as a promising candidate for anticancer research. |
体外活性 | PBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides[1]. |
分子量 | 272.73 |
分子式 | C15H13ClN2O |
CAS No. | 2819989-61-0 |
Smiles | O=C1C=2C(NC(N1)C3=CC(C)=CC=C3)=CC=CC2Cl |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (183.33 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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