2319611-93-1
中文名称
IACS-9571 hydrochloride
英文名称
IACS-9571 hydrochloride
CAS
2319611-93-1
分子式
C32H43ClN4O8S
分子量
679.23
MOL 文件
2319611-93-1.mol
2319611-93-1 结构式
物理化学性质
储存条件-20°C储存
溶解度DMSO: 125 mg/mL (184.03 mM)
形态Solid
颜色Light brown to brown
水溶解性Water: 10 mg/mL (14.72 mM)
常见问题列表
生物活性
IACS-9571 (ASIS-P040) hydrochloride 是溴结构域蛋白 TRIM24 和 BRPF1 的抑制剂，对 TRIM24 的 IC50 和 Kd 值分别为 8 nM 和 31 nM，对 BRPF1 的 Kd 值为 14 nM。靶点
IC50: 8 nM (TRIM24)
Kd: 31 nM (TRIM24), 14 nM (BRPF1)
体外研究
IACS-9571 Hydrochloride shows excellent cellular potency with EC 50 of 50 nM. IACS-9571 Hydrochloride (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 Hydrochloride is a selective dual TRIM24/BRPF1 inhibitor (K d =1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 Hydrochloride does not interact with the BET sub-family of bromodomains, displaying greater than 7700-fold selectivity versus BRD4 (1, 2) relative to TRIM24.