JNK3-IN-10
JNK3-IN-10 is a blood-brain barrier-impermeable JNK3 inhibitor (IC50=0.257 nM) with over 400-fold selectivity over JNK1. JNK3-IN-10 blocks the JNK3-mediated signaling pathway downstream of TGF-β1, inhibits TGF-β1-induced phosphorylation of c-Jun, reduces the expression of pro-fibrotic markers, and restores the expression of the epithelial protein E-cadherin. JNK3-IN-10 exhibits low cytotoxicity, anti-fibrotic, cytoprotective and renoprotective effects, and alleviates albuminuria, glomerulosclerosis and podocyte foot process fusion. JNK3-IN-10 can be used for the research of chronic kidney disease, glomerulosclerosis and adriamycin-induced nephropathy.
For research use only. We do not sell to patients.
- CAS No.: 3085181-00-3
- Formula: C24H24Cl2N8O2S
- Molecular Weight:559.47
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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
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hJNK3 0.257 nM (IC50) |
JNK3-IN-10 (Compound 14bg) (1 μM; pre-incubated for 20 min, co-incubated with ATP for 2 h) exhibits 84-fold, 472-fold and 194-fold selectivity over JNK1, JNK2 and p38α, respectively, and shows extremely low off-target kinase activity at the concentration of 1 μM[1].
JNK3-IN-10 (1 μM; 30 min; 37 °C) exhibits moderate microsomal stability in human liver microsomes, with 64.63% remaining after incubation at 37 °C for 30 min[1].
JNK3-IN-10 exhibits low blood-brain barrier (BBB) permeability, with a Pe value of 0.52×10-6 cm/s, and is classified as a non-BBB-permeable compound[1].
JNK3-IN-10 (5 μM; pre-incubated for 1 h) inhibits TGF-β1-induced c-Jun phosphorylation and the expression of pro-fibrotic markers (PAI-1, COL1α1) in differentiated human podocytes, without reducing cell viability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Differentiated human podocytes
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Concentration:5 μM
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Incubation Time:1 h pretreatment
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Result:Suppressed TGF-β1-induced phosphorylation of c-Jun.
Showed no cytotoxicity, with cell viability remaining at control levels.
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Cell Line:Differentiated human podocytes
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Concentration:5 μM
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Incubation Time:1 h pretreatment
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Result:Attenuated TGF-β1-induced upregulation of PAI-1 and COL1α1.
Restored E-cadherin expression to near-basal levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 8 weeks old, chronic kidney disease induced by single intravenous injection of Adriamycin at 12 mg/kg)[1]
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Dosage:2 mg/kg; 6 mg/kg
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Administration:i.p.; three times per week; 2 weeks
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Result:Significantly restored serum albumin levels and tended to reduce blood urea nitrogen (BUN) levels compared to untreated Adriamycin-injected mice.
Reduced urinary albumin-to-creatinine ratio, collagen-positive area, and glomerulosclerosis scores.
Decreased podocyte foot process effacement and preserved glomerular basement membrane structure.
Reduced Adriamycin-induced phosphorylation of c-Jun, suppressed upregulation of α-SMA and Col1α1, and partially restored E-cadherin expression in renal cortical tissues.
Downregulated fibrotic (α-SMA, Col1α1) and epithelial-mesenchymal transition-associated transcripts, with a trend toward recovery of podocyte-specific markers (E-cadherin, synaptopodin).
Showed no systemic toxicity.
Chemical Information
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CAS No. 3085181-00-3
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Molecular Weight 559.47
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Formula C24H24Cl2N8O2S
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SMILES
ClC1=C(C=CC(C2=C(N3C=C(SC3=N2)C(N)=O)C4=CC=NC(N[C@@H]5CCCN(C5)C(N(C)C)=O)=N4)=C1)Cl
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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)
JNK3-IN-10 Related Classifications
HY-181556 Related Classifications
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