JNK1 degrader-1 

JNK1 degrader-1 is a JNK1 HyT degrader. JNK1 degrader-1 can induce JNK1 degradation through the HyT-mediated ubiquitin-proteasome system and autophagy-lysosome pathway. JNK1 degrader-1 inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT). JNK1 degrader-1 can be used for research on fibrotic diseases and cancer metastasis. (Pink: JNK1 ligand (HY-183006); Blue: Hyt hydrophobic group (HY-W037848); Black: Linker (HY-B1008))^[1].

JNK1 degrader-1 (HY12) (10-100 nM; 5 h) inhibits the kinase activity of purified JNK1, with an inhibition rate of 86.01% at 100 nM and 59.55% at 10 nM^[1].
JNK1 degrader-1 (1 μM; 24-48 h) induces potent, dose- and time-dependent degradation of JNK1 in BEAS-2B cells via the ubiquitin-proteasome system and autophagy-lysosome pathway, with a DC₅₀ of 0.16 μM and a degradation rate of 70.40% after treatment at 1 μM for 48 h^[1].
JNK1 degrader-1 (1 μM; 48 h) selectively degrades JNK1 in BEAS-2B cells, with no significant effects on the protein levels of JNK2, p38 or ERK^[1].
JNK1 degrader-1 (0.1-1 μM; 1 h pre-treatment, 48 h total) inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT) in A549 cells, reverses the upregulation of mesenchymal markers and downregulation of epithelial markers at a concentration of 0.1 μM, and suppresses TGF-β1-induced JNK1 expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

575.50

C₂₉H₃₁BrN₆O₂

O=C(C1=CC=CC=C1NC2=C(Br)C=NC(NC3=CC=C(C(NCC45C[C@H](C6)C[C@H](C[C@H]6C5)C4)=O)C=C3)=N2)N

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• [1]. Huang Y, et al. Design, synthesis, and biological evaluation of novel hydrophobic tag-based degraders targeting JNK1. Bioorg Chem. 2026;174:109756.  [Content Brief]