| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
JNK3-IN-10 (14bg of compound) (1 μM; pre-incubated for 20 min, co-incubated with ATP for 2 h) showed selectivity of 84-fold, 472-fold, and 194-fold for JNK1, JNK2, and p38α, respectively, and exhibited extremely low off-target kinase activity at a concentration of 1 μM [1]. JNK3-IN-10 (1 μM; 30 min; 37 °C) showed moderate microsomal stability in human liver microsomes, with 64.63% remaining after incubation at 37 °C for 30 min [1]. JNK3-IN-10 has 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-incubation for 1 hour) inhibited the expression of TGF-β1-induced c-Jun phosphorylation and profibrotic markers (PAI-1, COL1α1) in differentiated human podocytes without reducing cell viability [1].
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|---|---|
| ln Vivo |
JNK3-IN-10 (compound 14bg) (2-6 mg/kg; intraperitoneal injection; three times a week; 2 weeks) significantly reduced doxorubicin-induced kidney damage, proteinuria, glomerular sclerosis and podocyte damage in male BALB/c mice, and had no systemic toxicity [1].
|
| Cell Assay |
ELISA assay [1]
Cell Types: Differentiated human podocytes Tested Concentrations: 5 μM Incubation Duration: 1 hour pretreatment Experimental Results: Inhibited TGF-β1-induced c-Jun phosphorylation. No cytotoxicity was observed, and cell viability remained at control levels. Western Blot Analysis [1] Cell Types: Differentiated human podocytes Tested Concentrations: 5 μM Incubation Duration: 1 hour of pretreatment Experimental Results: Reduced TGF-β1-induced upregulation of PAI-1 and COL1α1. Restored E-cadherin expression to near basal levels. |
| Animal Protocol |
Animal/Disease Models:BALB/c (male, 8 weeks old, chronic kidney disease induced by a single intravenous injection of 12 mg/kg doxorubicin) [1]
Doses: 2 mg/kg; 6 mg/kg Route of Administration: Intraperitoneal injection; three times a week; for 2 weeks Experimental Results: Compared with untreated doxorubicin-injected mice, serum albumin levels were significantly restored, and blood urea nitrogen (BUN) levels tended to decrease. The urine albumin/creatinine ratio, collagen-positive area, and glomerular sclerosis score were all reduced. The disappearance of podocyte foot processes was reduced, and the glomerular basement membrane structure was preserved. Doxorubicin-induced c-Jun phosphorylation levels were reduced, α-SMA and Col1α1 upregulation were inhibited, and the expression of E-cadherin in renal cortex was partially restored. Downregulation of fibrosis-related transcripts (α-SMA, Col1α1) and epithelial-mesenchymal transition-related transcripts was observed, with a trend toward recovery of podocyte-specific markers (E-cadherin, synaptic protein). No systemic toxicity was observed. |
| References |
| Molecular Formula |
C24H24CL2N8O2S
|
|---|---|
| Molecular Weight |
559.47
|
| CAS # |
3085181-00-3
|
| Appearance |
Typically exists as solids at room temperature
|
| 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
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7874 mL | 8.9370 mL | 17.8741 mL | |
| 5 mM | 0.3575 mL | 1.7874 mL | 3.5748 mL | |
| 10 mM | 0.1787 mL | 0.8937 mL | 1.7874 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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