IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1 , with an IC 50 of 8 nM for TRIM24, and K d s of 31 nM and 14 nM for TRIM24 and BRPF1 , respectively
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.