| Bioactivity | TRIM24/BRPF1-IN-2 (compound 20l) is a potent TRIM24/BRPF1 dual inhibitor, with IC50 values of 0.98 and 1.16 μM, respectively. TRIM24/BRPF1-IN-2 shows TRIM24/BRPF1 bromodomain binding affinity. TRIM24/BRPF1-IN-2 can be used for prostate cancer research[1]. |
| Invitro | TRIM24/BRPF1-IN-2 (compound 20l) (0-10 μM, 48 h) 抑制前列腺细胞系 (C4-2B、LNCaP 和 22Rv1) 的生长，IC50 值 分别为 0.78±0.15、1.07±0.47 和 0.82±0.26 μM[1]。TRIM24/BRPF1-IN-2抑制前列腺癌细胞基因和蛋白表达[1]。TRIM24/BRPF1-IN-2 表现出合理的 Caco-2 渗透性[1]。 RT-PCR[1] Cell Line: |
| In Vivo | TRIM24/BRPF1-IN-2 (compound 20l) (50 mg/kg，腹腔注射，每日1次，连用21天)可抑制肿瘤生长 (TGI = 53%) 而没有表现出明显的毒性[1]。 Animal Model: |
| Name | TRIM24/BRPF1-IN-2 |
| Formula | C20H22N2O4S |
| Molar Mass | 386.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Xiang Q, et al. Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. Eur J Med Chem. 2022 Jun 5;236:114311. |