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| 25mg |
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JNK Inhibitor VIII (TCS JNK 6o) is a selective and ATP-competitive inhibitor of the JNK-1, -2, and -3 c-Jun N-terminal kinases, with Kis of 2 nM, 4 nM, and 52 nM, respectively, and IC50 values of 45 nM and 160 nM for JNK-1 and -2, respectively.
| Targets |
JNK1 (Ki = 2 nM); JNK1 (IC50 = 45 nM); JNK2 (Ki = 4 nM); JNK2 (Ki = 160 nM); JNK3 (Ki = 52 nM)
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|---|---|
| ln Vitro |
TCS-JNK-6a binds to the ATP site in a competitive and reversible manner. This substance exhibits an impressive selectivity profile. In hepG2 cells, it also exhibits some inhibition of c-Jun phosphorylation. TCS-JNK-6o is a 2,5-dimethoxy analogue of TCS-JNK-6a in which the phenyl ring has been replaced by a dimethoxy group. TCS-JNK-6o exhibits additional increases in potency. [1]
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| ln Vivo |
JNK Inhibitor VIII (TCS-JNK-6o) pharmacokinetic profiles are established in Sprague-Dawley rats. The JNK Inhibitor VIII (TCS-JNK-6o) exhibits a brief half-life of about 1 h, rapid clearance, and hardly detectable bioavailability. Studies on microsomal incubation have shown that this compound has a very quick oxidative metabolism. [1]
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| Enzyme Assay |
Radioactive FlashPlates are used as the assay platform for Ser/Thr-kinase assays. In this format, biotinylated substrate peptide (2 μM), γ-[33P]-ATP (5 μM, 2 mCi/μmol), inhibitors (3-10000 nM in 2% DMSO), and enzyme are incubated for 1 h in buffer containing 25 mM Hepes, pH 7.5, 1 mM DTT, 10 mM MgCl2, 100 μM Na3VO4, and 0.075 mg/mL Triton X-100, stopped with 80 μL of stop buffer containing 100 mM EDTA and 4 M NaCl, transferred to streptavidin-coated 384-well FlashPlates, which are then washed 3 times and read using a TopCount microplate reader.
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| Cell Assay |
HepG2 human hepatoma cells (ATCC) are grown in low glucose MEM with 1×NEAA, 1×sodium pyruvate, and 10% FBS as dietary supplements. Cells are seeded at 5×104 cells/well in 500 μL of complete media on 24-well collagen-coated plates for P-c-Jun assays, and the plates are incubated overnight. The final inhibitor concentrations are provided by adding 5 μL directly to the media on the cells after serial compound dilutions in DMSO at 100×. Cells are stimulated for 30 minutes with TNFR or vehicle control after 1 hour, harvested in 70 μL of lysis buffer (TBS (54 mM Tris-HCl, pH 7.6, 150 mM NaCl), 1% TritonX-100,0.5% Nonidet P-40, 0.25% sodium deoxycholate, 1 mM EDTA, 1 mM EGTA, 0.5 mM sodium fluoride, 1 mM pervanadate, 1 μM microcystin, 1 mM AEBSF, 1 tablet of complete EDTA Free-Mini inhibitor cocktail) and then frozen at -80 degrees Celsius for use in the P-c-Jun assay.
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| Animal Protocol |
Sprague-Dawley rat
5 mg/kg IV, Oral gavage |
| References |
| Molecular Formula |
C₁₈H₂₀N₄O₄
|
|---|---|
| Molecular Weight |
356.38
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| Exact Mass |
356.15
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| Elemental Analysis |
C, 60.66; H, 5.66; N, 15.72; O, 17.96
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| CAS # |
894804-07-0
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| Related CAS # |
894804-07-0
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| Appearance |
Solid powder
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| SMILES |
CCOC1=C(C(=CC(=N1)NC(=O)CC2=C(C=CC(=C2)OC)OC)N)C#N
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| InChi Key |
KQMPRSZTUSSXND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20N4O4/c1-4-26-18-13(10-19)14(20)9-16(22-18)21-17(23)8-11-7-12(24-2)5-6-15(11)25-3/h5-7,9H,4,8H2,1-3H3,(H3,20,21,22,23)
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| Chemical Name |
N-(4-amino-5-cyano-6-ethoxypyridin-2-yl)-2-(2,5-dimethoxyphenyl)acetamide
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| Synonyms |
TCS-JNK-6o; TCS-JNK 6o; TCS JNK-6o; JNK Inhibitor VIII; c-Jun N-terminal Kinase Inhibitor VIII
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 71~250 mg/mL (199.2~701.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8060 mL | 14.0300 mL | 28.0599 mL | |
| 5 mM | 0.5612 mL | 2.8060 mL | 5.6120 mL | |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8060 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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