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Takinib (EDHS-206) TAK1 inhibitor

Name: Takinib (EDHS-206)
Brand: Selleck Chemicals
SKU: S8663
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S8663

Takinib 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.

Chemical Structure

Molecular Weight: 322.36

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Quality Control

Batch: S866301 DMSO]30 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.35%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.35

Related Targets	ERK p38 MAPK K-Ras Raf JNK MEK Ras S6 Kinase MAP4K Mixed Lineage Kinase
Other TAK1 Products	NG25 HS-276 Phospho-TAK1 (Ser439) Antibody [F17C11] TAB1 Antibody [M21E14] Phospho-TAK1 (Thr184/187) Antibody [G4C5] TAK1 Antibody [H23P12] TAK1 Antibody [P15P4]

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (93.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.370mg/ml (1.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.370mg/ml (1.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 7.4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	322.36	Formula	C₁₈H₁₈N₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1111556-37-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EDHS-206			Smiles	CCCN1C2=CC=CC=C2N=C1NC(=O)C3=CC=CC(=C3)C(=O)N

Mechanism of Action

Targets/IC₅₀/Ki	TAK1 (Cell-free assay) 9.5 nM IRAK4 (Cell-free assay) 120 nM IRAK1 (Cell-free assay) 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, this compound 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, this inhibitor treatment results in TNF-a-dependent induction of apoptosis due to inhibition of TAK1 as a key switch between survival and cell death. It does not inhibit any of the MAP2Ks or MAP3Ks family members, i.e., MKK6/MAP2K6, MEKK1/ MAP3K1, MKK1/MAP2K1. This chemical also shows no efficacy toward the TAK1-closely related MAP3K5/ASK1. It potently and selectively targets TAK1 and induces apoptosis in TNF-a-stimulated breast cancer and RA in vitro models.
In vivo	This compound slows tumor growth in the Hodgkin lymphoma xenograft NSG mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28820959/ [2] https://pubmed.ncbi.nlm.nih.gov/33139544/

Applications

Methods	Biomarkers	Images	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

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