in 1130

IN-1130 is a selective inhibitor of ALK5 with IC50 values of 5.3 nM, 36 nM, and 4.3 μM for phosphorylation of ALK5-mediated Smad3, ALK5 phosphorylation of casein and p38α mitogen-activated protein kinase.

BRPF1B TRIM24-IN-1 (compound 34) is a potent inhibitor of TRIM24, BRPF1, and BRPF2, with IC50 values of 0.43 μM, 0.34 μM, and 1.75 μM respectively. The dissociation constants (KD) for its binding with the bromodomains of TRIM24, BRPF1, and BRD1 are 222 nM, 137 nM, and 1130 nM respectively.