| Identification | Back Directory | [Name]
JNK-1-IN-4 | [CAS]
3047795-60-5 | [Synonyms]
JNK-1-IN-4
Benzamide, 2-[[5-bromo-2-[(4-methoxyphenyl)amino]-4-pyrimidinyl]amino]-5-[2-(dimethylamino)ethoxy]- | [Molecular Formula]
C22H25BrN6O3 | [MOL File]
3047795-60-5.mol | [Molecular Weight]
501.38 |
| Chemical Properties | Back Directory | [Boiling point ]
649.9±65.0 °C(predicted) | [density ]
1.442±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
15.35±0.50(predicted) |
| Hazard Information | Back Directory | [Uses]
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]. | [IC 50]
JNK1: 2.7 nM (IC50); JNK3: 9.0 nM (IC50); JNK2: 19.0 nM (IC50) | [References]
[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 |
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