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Takinib

Catalog No. T4264 CAS 1111556-37-6

Synonyms: EDHS-206

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Takinib, CAS 1111556-37-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 66.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 230.00
50 mg	In stock	$ 345.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.18%

Purity: 98.24%

Biological Description

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Storage & Solubility Information

Description	Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).
Targets&IC50	TAK1:9.5 nM
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.
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.
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.

Synonyms	EDHS-206
Molecular Weight	322.36
Formula	C18H18N4O2
CAS No.	1111556-37-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 1.61 mg/ml (5 mM), Sonication is recommended.

References and Literature

1. Totzke J, et al. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17;24(8):1029-1039. 2. Da Q, Yan Z, Li Z, et al. TAK1 is involved in sodium L-lactate-stimulated p38 signaling and promotes apoptosis[J]. Molecular and Cellular Biochemistry. 2020: 1-10.

Citations

1. Da Q, Yan Z, Li Z, et al. TAK1 is involved in sodium L-lactate-stimulated p38 signaling and promotes apoptosis. Molecular and Cellular Biochemistry. 2020: 1-10

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Parasitic Compound Library HIF-1 Signaling Pathway Compound Library Anti-Prostate Cancer Compound Library NO PAINS Compound Library Osteogenesis Compound Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Takinib 1111556-37-6 Apoptosis MAPK EDHS 206 HepG2 malaria MAP kinase kinase kinase, MEKK, MAPKKK cancer RASF Inhibitor arthritis inhibit EDHS-206 HuH7 RA-FLS EDHS206 MAP3K inhibitor

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