IACS-9571 (ASIS-P040) hydrochloride 是溴结构域蛋白 TRIM24 和 BRPF1 的抑制剂，对 TRIM24 的 IC₅₀ 和 K_d 值分别为 8 nM 和 31 nM，对 BRPF1 的 K_d 值为 14 nM。

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.

Solid

IC50: 8 nM (TRIM24)
Kd: 31 nM (TRIM24), 14 nM (BRPF1)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 125 mg/mL (184.03 mM; Need ultrasonic and warming)H₂O : 10 mg/mL (14.72 mM; Need ultrasonic)配制储备液