| Name | Takinib |
| Description | Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM). |
| Cell Research | MDA-MB-231 cells (1,000 cells/well) are seeded in a 96-well plate with 10% FBS, 5% Pen/Strep, 4 g/L glucose DMEM medium. After 24h, cells are serum starved with 1% FBS, 5% Pen/Strep, 4 g/L glucose DMEM medium for 4h. Cells are treated with titrations of Takinib in the presence or absence of 30 ng/mL TNFα. Plates at 0 h and 24 h following treatment are frozen at -80°C after removal of media. After 24 h, 100 μL ddH2O is added to each well and plates are refrozen. 1 μL from Hoechst stock [1 mg/mL in 1:4 DMSO/H2O] is dissolved in 1 mL of TNE buffer (10 mM Tris, 2 M NaCl, 1 mM Na2EDTA) and 100 μL of this solution is added to each well. The fluorescence is determined at 355/460 nm. |
| Kinase Assay | TAK1-TAB1 (50 ng/well) is incubated with 5 μM ATP containing radiolabeled [32P]-ATP in the presence of 300 mM substrate peptide (RLGRDKYKTLRQIRQ) in a final volume of 40 μL in the presence of buffer (containing 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1% β-Mercaptoethanol, 10 mM magnesium acetate, 0.5 mM MnCl) and indicated compounds. The reaction is let go for 10 min and stopped with 10 μL concentrated H3PO4. |
| In vitro | Takinib reduces phosphorylation significantly but does not influence total protein levels. Takinib inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun in a dose-dependent manner. Takinib(10 mM) shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 1.61 mg/mL (4.99 mM), Sonication is recommended.
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| Keywords | Takinib | TAK1 | RASF | RA-FLS | MAP3K | MAP kinase kinase kinase, MEKK, MAPKKK | malaria | Inhibitor | inhibit | HuH7 | HepG2 | EDHS206 | EDHS 206 | cancer | arthritis | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Reprogramming Compound Library | Anti-Parasitic Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Kinase Inhibitor Library | Inhibitor Library | NO PAINS Compound Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Active Compound Library |
United States
