1800477-30-8

1800477-30-8 structure

Name: IACS-9571
Chemical Name: IACS-9571
CAS Number: 1800477-30-8
Molecular Formula: C₃₂H₄₂N₄O₈S
Molecular Weight: 642.76
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-01-29 09:23:52
Modify Date: 2024-01-02 06:37:40
IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

Name	IACS-9571

Description	IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Research Areas >> Cancer
Target	IC50: 8 nM (TRIM24)[1] Kd: 31 nM (TRIM24), 14 nM (BRPF1)[1]
In Vitro	IACS-9571 shows excellent cellular potency with EC50 of 50 nM. IACS-9571 (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 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 does not interact with the BET sub-family of bromodomains, displaying greater than 7,700-fold selectivity versus BRD4(1, 2) relative to TRIM24[1].
References	[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.