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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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JNK1 10 nM (DC50) |
Cereblon |
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.
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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.
| Species | Dose | Route | T1/2 | Cmax |
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| Rat[1] | 75 mg/kg | p.o. | 6.4 h | 0.5 μM |
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC JNK1 Degrader-1 Related Classifications
HY-170601 Related Classifications
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