| Bioactivity | BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects[1]. |
| Invitro | BRD4/NAMPT-IN-1 对 BET 家族其他成员的 IC50 为 12 nM (BRD4(BD1))和 41 nM(BRD4(BD2))[1]。BRD4/NAMPT-IN-1 抑制癌细胞增殖的 IC50 分别为 2.37 μM (Hep3B)， 6.49 μM (Huh7)， 5.44 μM (HCCLM3) 和 9.51 μM (LX-2)[1]。BRD4/NAMPT-IN-1 (1-10 μM; 72 h) 处理 Hep3B 细胞发现：可以抑制 BRD4 上调的癌基因的表达，同时降低了 NAPRT 和 NAMPT 的水平；显著增加细胞在 G0/G1 阶段的停滞；剂量依赖性的诱导细胞凋亡；剂量依赖性的抑制细胞的迁移能力[1]。BRD4/NAMPT-IN-1 (1-10 μM; 72 h) 剂量依赖性地降低了 Hep3B 细胞和 HCCLM3 细胞中 NAD + 的浓度[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> BRD4/NAMPT-IN-1 相关抗体: Apoptosis Analysis[1] Cell Line: |
| In Vivo | BRD4/NAMPT-IN-1 (i.p.; 40 mg/kg/day 和 80 mg/kg/day; 持续 27 天) 在 HCCLM3 异种移植裸鼠体内表现出剂量依赖的肿瘤抑制效果[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C30H30ClN7O2S |
| Molar Mass | 588.12 |
| 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]. Yin C, et al. Discovery of potent and novel dual NAMPT/BRD4 inhibitors for efficient treatment of hepatocellular carcinoma. Eur J Med Chem. 2024 May 5;271:116444. |