PROTAC JNK1 Degrader-2
PROTAC JNK1 Degrader-2 is a VHL-recruiting JNK1 PROTAC degrader with a DC50 of 4.90 nM. It selectively induces JNK1 degradation via the VHL-dependent ubiquitin-proteasome pathway and inhibits TGF-β1-induced epithelial-mesenchymal transition. PROTAC JNK1 Degrader-2 can be used for research on organ fibrosis and tumor metastasis.
(Pink: JNK1 Target protein ligand; Blue: VHL E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Formula: C57H72BrN11O7
- Molecular Weight:1103.16
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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
Biological Activity
Description
IC50 & Target
[1]|
JNK1 4.9 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BEAS-2B | DC50 |
4.90 nM
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Degradation of JNK1 in human BEAS-2B cells assessed by western blot analysis after 12 hrs of treatment.
Degradation of JNK1 in human BEAS-2B cells assessed by western blot analysis after 12 hrs of treatment.
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42612267 |
In Vitro
PROTAC JNK1 Degrader-2 (compound YC2) (10-100 nM; 60 min) inhibits recombinant JNK1 kinase activity by 58.77% at 100 nM and 44.35% at 10 nM[1].
PROTAC JNK1 Degrader-2 (1-50 nM; 12 h) selectively degrades JNK1 in BEAS-2B cells without affecting the expression of JNK2, p38α, and ERK[1].
PROTAC JNK1 Degrader-2 (1-500 nM; 12 h) induces JNK1 degradation in BEAS-2B cells in a concentration-dependent manner with a DC50 of 4.90 nM[1].
PROTAC JNK1 Degrader-2 (0.01 μM; 24 h) promotes the degradation of JNK1 in BEAS-2B cells through the VHL-dependent ubiquitin-proteasome pathway[1].
PROTAC JNK1 Degrader-2 (0.1 μM; 2-48 h) induces rapid and sustained degradation of JNK1 in BEAS-2B cells[1].
PROTAC JNK1 Degrader-2 (0.1-1 μM; 1 h) attenuates TGF-β1-induced EMT in A549 cells[1].
PROTAC JNK1 Degrader-2 (10 μM; 5-120 min) exhibits acceptable metabolic stability in human liver microsomes with a half-life of 57.4 min, and a half-life of 123.1 min in mouse liver microsomes[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
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Concentration:1, 5, 10, 50 nM
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Incubation Time:12 h
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Result:Efficiently degraded JNK1 in a concentration-dependent manner.
Displayed the greatest specificity for JNK1, causing only limited degradation of JNK2, particularly at concentrations of 1-5 nM.
Did not affect the expression of p38α and ERK.
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Cell Line:BEAS-2B
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Concentration:1, 5, 10, 50, 100, 500 nM
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Incubation Time:12 h
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Result:Resulted in a concentration-dependent decrease in JNK1 protein levels.
Achieved nearly complete degradation at 50 nM.
Calculated DC50 of 4.90 nM.
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Cell Line:BEAS-2B
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Concentration:0.01 μM
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Incubation Time:24 h
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Result:Pretreatment with MG132 markedly rescued JNK1 protein levels.
Inhibition of Cullin-RING E3 ligase activity by MLN4924 substantially attenuated JNK1 degradation.
Pretreatment with excess free VHL ligand effectively blocked PROTAC JNK1 Degrader-2-mediated JNK1 degradation.
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Cell Line:BEAS-2B
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Concentration:0.1 μM
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Incubation Time:2, 4, 6, 8, 12, 24, 48 h
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Result:Induced rapid and sustained degradation of JNK1.
JNK1 protein levels began to decline as early as 2 h after treatment and were markedly reduced by 4-6 h.
More than 90% of JNK1 was degraded after 12 h of treatment, and this level of degradation was maintained for at least 48 h.
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Cell Line:A549
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Concentration:0.1, 0.5, 1 μM
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Incubation Time:1 h
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Result:Dose-dependently reversed TGF-β1-induced changes: fibronectin expression was suppressed, and E-cadherin levels were restored.
At 1 μM, exhibited efficacy comparable to that of nintedanib (1 μM).
Degraded JNK1 in this model.
Chemical Information
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Molecular Weight 1103.16
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Formula C57H72BrN11O7
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SMILES
O=C(N)C1=CC=CC=C1NC2=C(Br)C=NC(NC3=CC=C(C(N4CC(C5)N(CCCCCCCCCC(N[C@@H](C(N6[C@H](C(N[C@H](C7=CC=C(C8=C(C)N=C(C)O8)C=C7)C)=O)C[C@@H](O)C6)=O)C(C)(C)C)=O)C5C4)=O)C=C3)=N2
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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-2 Related Classifications
HY-189269 Related Classifications
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