Product Details
Product Name:
Takinib |
CAS No.:
1111556-37-6 |
Purity:
99.18% |
Supply Ability:
10g |
Release date:
2024/11/17 |
Product Introduction
Bioactivity
名稱 | Takinib |
描述 | Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM). |
細(xì)胞實(shí)驗(yàn) | 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. |
激酶實(shí)驗(yàn) | 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. |
體外活性 | 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. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 1.61 mg/ml (5 mM ), Sonication is recommended.
|
關(guān)鍵字 | EDHS 206 | HepG2 | malaria | MAP kinase kinase kinase, MEKK, MAPKKK | cancer | RASF | Inhibitor | arthritis | inhibit | HuH7 | Apoptosis | RA-FLS | Takinib | EDHS206 | MAP3K |
相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
相關(guān)庫 | 細(xì)胞凋亡化合物庫 | 抗寄生蟲庫 | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抑制劑庫 | 抗前列腺癌化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$1.00/1g |
VIP6Y
|
Career Henan Chemical Co
|
2019-12-23 |