BAZ1A-IN-1 是一种有效的 BAZ1A（含溴结构域蛋白）抑制剂。 BAZ1A-IN-1 对 BAZ1A 溴结构域的 KD 值为 0.52 μM。BAZ1A-IN-1 对高表达 BAZ1A 的癌细胞系显示出良好的抗生存活性，但对低表达 BAZ1A 的癌细胞表现出弱活性或无活性。
货号:ajcx36178
CAS:941521-45-5
分子式:C16H12N4O3S
分子量：340.36
溶解度:DMSO : 83.33 mg/mL (244.83 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A[1].

BAZ1A-IN-1 (Cpd-2) (0.015-100 μM; 96 hours) exhibits good anti-viability activity against all the four cancer cell lines that have a high expression level of BAZ1A, with IC50 values of 5.08 μM, 4.29 μM, 10.65 μM, and 7.70 μM for THP-1, ZR-75-30, BT474, and H1975 cells, respectively[1].

[1]. Yang Z, et al. Discovery of BAZ1A bromodomain inhibitors with the aid of virtual screening and activity evaluation. Bioorg Med Chem Lett. 2021;33:127745.