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Synonyms | TCS JNK 6o | Storage (From the date of receipt) |
3 years -20°C powder | ||||||||
化学式 | C18H20N4O4 |
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分子量 | 356.38 | CAS No. | 894804-07-0 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 71 mg/mL (199.22 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. |
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in vitro | TCS-JNK-6a binds competitively and reversibly to the ATP site. This compound demonstrates a remarkable selectivity profile. Additionally, it shows some inhibition of c-Jun phosphorylation in hepG2 cells. TCS-JNK-6o is a 2,5-dimethoxy analogue of TCS-JNK-6a with the dimethoxy substitution of the phenyl ring. TCS-JNK-6o shows further gains in potency.[1] |
in vivo | Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. JNK Inhibitor VIII (TCS-JNK-6o) showes a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism is very rapid with this compound.[1] |
キナーゼアッセイ | Ser/Thr-kinase | |
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Ser/Thr-kinase assays are performed using a radioactive FlashPlate-based assay platform. 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. | ||
細胞アッセイ | 細胞株 | hepG2 cells |
濃度 | Serial concentrations | |
反応時間 | 1 h | |
実験の流れ | HepG2 human hepatoma cells (ATCC) are cultured in low glucose MEM supplemented with 1×NEAA, 1×sodium pyruvate, and 10% FBS. For P-c-Jun assays, cells are plated at 5×104 cells/well in 500 μL of complete media on 24-well collagen-coated plates and incubated overnight. Serial compound dilutions are made in DMSO at 100×, and then 5 μL is added directly to the media on the cells to provide the final inhibitor concentrations. After 1 h, cells are stimulated with vehicle control or TNFR for 30 min and harvested in 70μL 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 frozen at -80 °C prior to use in the P-c-Jun assay. |
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動物実験 | 動物モデル | Sprague-Dawley rat |
投薬量 | 5 mg/kg | |
投与方法 | IV, Oral gavage |
Blocking GSDME-mediated pyroptosis in renal tubular epithelial cells alleviates disease activity in lupus mice [ Cell Death Discov, 2022, 8(1):113] | PubMed: 35279675 |
Dabrafenib Promotes Schwann Cell Differentiation by Inhibition of the MEK-ERK Pathway [ Molecules, 2021, 26(8)2141] | PubMed: 33917810 |
Inhibition of JNK signaling in the Asian malaria vector Anopheles stephensi extends mosquito longevity and improves resistance to Plasmodium falciparum infection [ PLoS Pathog, 2018, 14(11):e1007418] | PubMed: 30496310 |
Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells [ PLoS One, 2015, 10(11):e0143685] | PubMed: 26606677 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。