PROTAC JNK1 Degrader-1
PROTAC JNK1 Degrader-1 is a JNK1 PROTAC degrader with a DC50 of 10 nM. PROTAC JNK1 Degrader-1 reduces the level of fibronectin. PROTAC JNK1 Degrader-1 can be used for the research of pulmonary fibrosis.
(Pink: JNK1 ligand (HY-170602); Blue: Cereblon ligand (HY-41547); Black: linker (HY-40178)).
For research use only. We do not sell to patients.
- Formula: C35H32BrN9O6
- Molecular Weight:754.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
JNK1 10 nM (DC50) |
Cereblon |
In Vitro
PROTAC JNK1 Degrader-1 (Compound PA2) (0.01-1 μM; 48 h) induces dose-dependent degradation of JNK1 in BEAS-2B cells, with a maximum degradation rate of 99.5% at the concentration of 0.1 μM, while a hook effect occurs at 1 μM[1].
PROTAC JNK1 Degrader-1 (10 nM, 100 nM; 12-48 h) induces the degradation of JNK1 in BEAS-2B cells via the CRBN- and proteasome-dependent ubiquitination pathway[1].
PROTAC JNK1 Degrader-1 (30 nM; 49 h) attenuates TGF-β1-induced epithelial-mesenchymal transition (EMT) and reduces fibronectin levels in A549 cells at a concentration of 30 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:BEAS-2B normal human lung epithelial cells
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Concentration:0.01 μM, 0.1 μM, 1 μM
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Incubation Time:48 h
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Result:Induced JNK1 degradation rate of 98.9 % at 0.01 μM.
Induced JNK1 degradation rate of 99.5 % at 0.1 μM.
Induced JNK1 degradation rate of 90.4 % at 1 μM.
Showed a dose-dependent trend with a Hook Effect observed at 1 μM.
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Cell Line:BEAS-2B normal human lung epithelial cells
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Concentration:10 nM (CHX pre-treatment); 100 nM (MG-132, Pomalidomide, MLN4924 pre-treatment)
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Incubation Time:48 h (CHX pre-treatment); 12 h (MG-132, Pomalidomide, MLN4924 pre-treatment)
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Result:Enhanced PA2-induced JNK1 degradation when cells were pre-treated with CHX.
Significantly blocked or weakened PA2-induced JNK1 degradation when cells were pre-treated with MG-132, Pomalidomide, or MLN4924.
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Cell Line:BEAS-2B normal human lung epithelial cells
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Concentration:1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
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Incubation Time:12 h
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Result:Induced degradation of JNK1 in a concentration-dependent manner.
Did not affect the expression levels or induce degradation of JNK2, p38, or ERK proteins.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:30 nM
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Incubation Time:1 h pre-incubation, followed by 48 h incubation with TGF-β1
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Result:Reduced the elevated Fibronectin protein levels induced by TGF-β1, an effect similar to that of 1 μM Nintedanib.
Concurrent with JNK1 degradation.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax |
|---|---|---|---|---|
| Rat[1] | 75 mg/kg | p.o. | 6.4 h | 0.5 μM |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 754.59
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Formula C35H32BrN9O6
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SMILES
O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)C4=CC=C(NC5=NC=C(Br)C(NC6=CC=CC=C6C(N)=O)=N5)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)