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Takinib

SKU: orb1303009

Description

Takinib

Research Area

Cell Biology, Signal Transduction

Images & Validation

Key Properties

CAS Number1111556-37-6
MW322.36
Purity98.29%
FormulaC18H18N4O2
SMILESCCCn1c(NC(=O)c2cccc(c2)C(N)=O)nc2ccccc12
TargetApoptosis,MAPK
SolubilityDMSO:1.61 mg/mL (4.99 mM)

Bioactivity

Target IC50
IRAK4:120 nM|IRAK1:390 nM|GCK:430 nM|MINK1:1.9 μM|TAK1:9.5 nM|CLK2:430 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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

cancer, arthritis, Apoptosis, EDHS 206, EDHS206, EDHS-206, HuH7, Inhibitor, HepG2, malaria, MAP kinase kinase kinase, MEKK, MAPKKK, MAP3K, inhibit, RASF, RA-FLS, Takinib, TAK1

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Key Properties

No computed properties available.

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Takinib (orb1303009)

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5 mg
$ 110.00
10 mg
$ 170.00
25 mg
$ 270.00
50 mg
$ 390.00
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