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Synonyms:
JNK3-IN-10
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | JNK3-IN-10 is a JNK3 inhibitor that does not penetrate the blood-brain barrier and has an IC50 of 0.257 nM, exhibiting over 400-fold selectivity for JNK1. It 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 epithelial protein E-cadherin (E-cadherin) expression. JNK3-IN-10 demonstrates low cytotoxicity and offers antifibrotic, cytoprotective, and renoprotective effects, alleviating albuminuria, glomerulosclerosis, and podocyte foot process fusion. It is applicable in research on chronic kidney disease, glomerulosclerosis, and adriamycin-induced nephropathy. |
| Targets & IC50 | JNK3 (human):0.257 nM |
| In vitro | JNK3-IN-10 (Compound 14bg) exhibits a 84-fold, 472-fold, and 194-fold selectivity for JNK1, JNK2, and p38α, respectively, with minimal off-target kinase activity at a concentration of 1 μM, following pre-incubation for 20 minutes and co-incubation with ATP for 2 hours. At 1 μM concentration and 37 °C, JNK3-IN-10 shows moderate microsomal stability in human liver microsomes, retaining 64.63% after a 30-minute incubation. Its permeability through the blood-brain barrier (BBB) is low, with a P e value of 0.52×10^-6 cm/s, classifying it as a BBB non-permeable compound. Additionally, JNK3-IN-10 at 5 μM, pre-incubated for 1 hour, effectively inhibits TGF-β1-induced phosphorylation of c-Jun and the expression of profibrotic markers (PAI-1, COL1α1) in differentiated podocytes, without reducing cell viability. |
| In vivo | JNK3-IN-10 (Compound 14bg) (2-6 mg/kg; i.p.; three times a week; 2 weeks) significantly alleviates doxorubicin-induced nephropathy, albuminuria, glomerulosclerosis, and podocyte damage in male BALB/c mice, without exhibiting systemic toxicity. |
| Molecular Weight | 559.47 |
| Formula | C24H24Cl2N8O2S |
| Cas No. | 3085181-00-3 |
| Smiles | C(N)(=O)C1=CN2C(=C(N=C2S1)C3=CC(Cl)=C(Cl)C=C3)C4=NC(N[C@H]5CN(C(N(C)C)=O)CCC5)=NC=C4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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