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8nM和31nM，对BRPF1的Kd值为14nM。
货号:ajcx30792
CAS:2319611-93-1
分子式:C32H43ClN4O8S
分子量：679.22
溶解度:DMSO: 125 mg/mL (184.03 mM); H2O: 10 mg/mL (14.72 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively[1].

IACS-9571 Hydrochloride shows excellent cellular potency with EC50 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 (Kd=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[1].

[1]. Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54.