2. PROTAC MAPK/ERK Pathway
  3. PROTACs JNK
  4. 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)).

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PROTAC JNK1 Degrader-1

PROTAC JNK1 Degrader-1 화학구조

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PROTAC JNK1 Degrader-1 Related Antibodies

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  • Biological Activity

  • 순도&문서

  • References

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제품 설명

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[1]. (Pink: JNK1 ligand (HY-170602); Blue: Cereblon ligand (HY-41547); Black: linker (HY-40178)).

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.

PROTAC JNK1 Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: BEAS-2B normal human lung epithelial cells
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: BEAS-2B normal human lung epithelial cells
Concentration: 10 nM (CHX pre-treatment); 100 nM (MG-132, Pomalidomide, MLN4924 pre-treatment)
Incubation Time: 48 h (CHX pre-treatment); 12 h (MG-132, Pomalidomide, MLN4924 pre-treatment)
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.

Western Blot Analysis[1]

Cell Line: BEAS-2B normal human lung epithelial cells
Concentration: 1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM
Incubation Time: 12 h
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.

Western Blot Analysis[1]

Cell Line: A549 human lung adenocarcinoma cells
Concentration: 30 nM
Incubation Time: 1 h pre-incubation, followed by 48 h incubation with TGF-β1
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

PROTAC JNK1-targeted-1 (Compound PA2) (75 mg/kg; p.o.; single dose) exhibits an elimination half-life of 6.4 h and a maximum blood concentration of 0.5 μM following administration to male Sprague-Dawley rats[1].

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

754.59

화학식

C35H32BrN9O6
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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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PROTAC JNK1 Degrader-1 Related Classifications

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Keywords:

PROTAC JNK1 Degrader-1PROTACsJNKc-Jun N-terminal kinaseproteasomal degradationERKpulmonary fibrosisJNK2p38JNK1A549 cellsCRBNubiquitination pathwayBEAS-2B cellsInhibitorinhibitorinhibit

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상품명:
PROTAC JNK1 Degrader-1
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HY-170601
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