2. MAPK/ERK Pathway TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. JNK TGF-beta/Smad Cadherin
  4. 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.

JNK3-IN-10

JNK3-IN-10 Chemical Structure

CAS No. : 3085181-00-3

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JNK3-IN-10 Related Antibodies

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Description

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[1].

IC50 & Target[1]

hJNK3

0.257 nM (IC50)

In Vitro

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.

JNK3-IN-10 Related Antibodies

ELISA Assay[1]

Cell Line: Differentiated human podocytes
Concentration: 5 μM
Incubation Time: 1 h pretreatment
Result: Suppressed TGF-β1-induced phosphorylation of c-Jun.
Showed no cytotoxicity, with cell viability remaining at control levels.

Western Blot Analysis[1]

Cell Line: Differentiated human podocytes
Concentration: 5 μM
Incubation Time: 1 h pretreatment
Result: Attenuated TGF-β1-induced upregulation of PAI-1 and COL1α1.
Restored E-cadherin expression to near-basal levels.
Parmacokinetics
Species Dose Route AUC0-t Cmax T1/2 CL Bioavailability
Mice[1] 1 mg/kg i.v. 614 ng·h/mL 1115.01 ng/mL 0.21 h 204 mL/min/kg /
Mice[1] 3 mg/kg p.o. 392 ng·h/mL 378 ng/mL 0.34 h / 21.3 %
Mice[1] 1 mg/kg i.p. 718 ng·h/mL 136 ng/mL 1.14 h 129.63 mL/min/kg /
In Vivo

JNK3-IN-10 (Compound 14bg) (2-6 mg/kg; i.p.; three times per week; 2 weeks) significantly alleviates Adriamycin (HY-15142A)-induced renal injury, albuminuria, glomerulosclerosis, and podocyte damage in male BALB/c mice, with no systemic toxicity[1].

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

Animal Model: BALB/c (male, 8 weeks old, chronic kidney disease induced by single intravenous injection of Adriamycin at 12 mg/kg)[1]
Dosage: 2 mg/kg; 6 mg/kg
Administration: i.p.; three times per week; 2 weeks
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.
Molecular Weight

559.47

Formula

C24H24Cl2N8O2S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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JNK3-IN-10 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNK3-IN-103085181-00-3JNKTGF-beta/SmadCadherinc-Jun N-terminal kinaseTransforming growth factor betaJNK3E-cadherinp38αJNK2JNK1adriamycin-induced nephropathyTGF-β1c-Junglomerulosclerosischronic kidney diseaseInhibitorinhibitorinhibit

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