Takinib

For research use only.

Catalog No.S8663 Synonyms: EDHS-206

1 publication

Takinib Chemical Structure

CAS No. 1111556-37-6

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.

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Selleck's Takinib has been cited by 1 publication

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Choose Selective TAK1 Inhibitors

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; 

PubMed: 28820959     


B Time course analysis of TNF signaling downstream of TAK1. Cells were treated with 10μM Takinib and stimulated with TNF for indicated time. Phosphorylated and total IKK, p-38 and p-65 were detected via Western blot analysis. GAPDH was measured as a loading control. C Dose-dependent effects of TAK1 downstream signaling in TNF-activated cells.

28820959

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 64 mg/mL (198.53 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 322.36
Formula

C18H18N4O2

CAS No. 1111556-37-6
Storage powder
in solvent
Synonyms EDHS-206
Smiles CCCN1C2=CC=CC=C2N=C1NC(=O)C3=CC=CC(=C3)C(=O)N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID