Takinib (Standard)
Takinib (Standard) is the analytical standard of Takinib. This product is intended for research and analytical applications. Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=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 is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).
For research use only. We do not sell to patients.
- CAS No.: 1111556-37-6
- Formula: C18H18N4O2
- Molecular Weight:322.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Product Information
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Chemical Information
- Purity & Documentation
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Help & FAQs
Product Information
The compound is the grade of analytical standard, which is the reference standard supplied assay. It is commonly used in qualitative, quantitative and methodological research experiments in HPLC, GC and MS.
Chemical Information
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CAS No. 1111556-37-6
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Molecular Weight 322.36
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Formula C18H18N4O2
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SMILES
CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=O
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Synonyms
EDHS-206 (Standard)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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. [Content Brief]
[2]. Scarneo SA, et.al. Pharmacological inhibition of TAK1, with the selective inhibitor takinib, alleviates clinical manifestation of arthritis in CIA mice. Arthritis Res Ther. 2019 Dec 17;21(1):292. [Content Brief]
[3]. Raphemot R, et al. Plasmodium PK9 Inhibitors Promote Growth of Liver-Stage Parasites. Cell Chem Biol. 2019 Mar 21;26(3):411-419.e7. [Content Brief]
[4]. Panipinto PM, et.al. Takinib Inhibits Inflammation in Human Rheumatoid Arthritis Synovial Fibroblasts by Targeting the Janus Kinase-Signal Transducer and Activator of Transcription 3 (JAK/STAT3) Pathway. Int J Mol Sci. 2021;22(22):12580. Published 2021 Nov 22. [Content Brief]
[5]. Song Z,et.al. Essential role of the linear ubiquitin chain assembly complex and TAK1 kinase in A20 mutant Hodgkin lymphoma. Proc Natl Acad Sci U S A. 2020 Nov 17;117(46):28980-28991. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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