JNK-1-IN-4

JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models[1].

JNK1: 2.7 nM (IC₅₀); JNK3: 9.0 nM (IC₅₀); JNK2: 19.0 nM (IC₅₀)

[1] Huang Y, et al., Structure Optimization of c-Jun N-terminal Kinase 1 Inhibitors for Treating Idiopathic Pulmonary Fibrosis. J Med Chem. 2024 Oct 10;67(19):17713-17737. DOI:10.1021/acs.jmedchem.4c01764