Home MAPK TAK1 inhibitor - Apoptosis related activator - IRAK inhibitor Takinib (EDHS-206)

Takinib (EDHS-206)

Catalog No.S8663

For research use only.

Takinib (EDHS-206) is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib induces apoptosis.

Takinib (EDHS-206) Chemical Structure

CAS No. 1111556-37-6

Selleck's Takinib (EDHS-206) has been cited by 4 Publications

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Biological Activity

Description Takinib (EDHS-206) is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib induces apoptosis.
Targets
TAK1 [1]
(Cell-free assay)		 IRAK4 [1]
(Cell-free assay)		 IRAK1 [1]
(Cell-free assay)
9.5 nM 120 nM 390 nM
In vitro

Takinib is an inhibitor of autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation. At 10 μM, Takinib shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. TAK1/MAP3K7 is most potently inhibited with a half maximal inhibitory concentration (IC50) value of 9.5 nM. In cell models of rheumatoid arthritis and metastatic breast cancer, Takinib treatment results in TNF-a-dependent induction of apoptosis due to inhibition of TAK1 as a key switch between survival and cell death. Takinib does not inhibit any of the MAP2Ks or MAP3Ks family members, i.e., MKK6/MAP2K6, MEKK1/ MAP3K1, MKK1/MAP2K1. Takinib also shows no efficacy toward the TAK1-closely related MAP3K5/ASK1. Takinib potently and selectively targets TAK1 and induces apoptosis in TNF-a-stimulated breast cancer and RA in vitro models[1].

Assay
Methods Test Index PMID
Western blot p-IKK / IKK / p-p38 / p-38 / p-p65 / p-65 / p-c-Jun / c-Jun / p-MAPK9 / MAPK9 / p-MAPK8 / MAPK8 28820959

Protocol (from reference)

Cell Research:

[1]
  • Cell lines: MDA-MB-231 cells
  • Concentrations: --
  • Incubation Time: 24 h
  • Method:

    MDA-MB-231 cells (1,000 cells/well) are seeded in a 96-well plate with 10% FBS, 5% Pen/Strep, 4g/l glucose DMEM medium. After 24h, cells are serum starved with 1% FBS, 5% Pen/Strep, 4g/l glucose DMEM medium for 4h. Cells are treated with titrations of Takinib in the presence or absence of 30 ng/mL TNFa. Plates at 0h and 24h following treatment were frozen at -80℃ after removal of media. After 24h, 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 (10mM Tris, 2M NaCl, 1 mM Na2EDTA) and 100 μl of this solution is added to each well. The fluorescence is determined at 355/460 nm.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 322.36
Formula

C18H18N4O2
CAS No. 1111556-37-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCN1C2=CC=CC=C2N=C1NC(=O)C3=CC=CC(=C3)C(=O)N

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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