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Merck
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Key Documents

SML2216

Sigma-Aldrich

Takinib

≥98% (HPLC)

Synonyme(s) :

N1-(1-Propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide

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About This Item

Formule empirique (notation de Hill):
C18H18N4O2
Numéro CAS:
Poids moléculaire :
322.36
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

CCCN1C2=CC=CC=C2N/C1=N\C(C3=CC(C(N)=O)=CC=C3)=O

Description générale

Takinib belongs to the aminobenzimidazole class of inhibitors.

Application

Takinib has been used as an inhibitor of transforming 28 growth factor - β-activated kinase -1 (TAK-1) in human leukemia monocytic THP-1 cells. It may be used as a TAK1 inhibitor in Jurkat cells.

Actions biochimiques/physiologiques

Takinib is a selective inhibitor of TAK1/MAP3K7 kinase, which is a member of the MAP3K family and a key regulator of cell death. It binds in the TAk1 ATPbinding pocket with an IC50 value of 9.5 nM. Takinib selectively induced apoptosis following TNF-α stimulation in rheumatoid arthritis and breast cancer.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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Consulter la Bibliothèque de documents

Juliane Totzke et al.
Cell chemical biology, 24(8), 1029-1039 (2017-08-19)
Tumor necrosis factor alpha (TNF-α) has both positive and negative roles in human disease. In certain cancers, TNF-α is infused locally to promote tumor regression, but dose-limiting inflammatory effects limit broader utility. In autoimmune disease, anti-TNF-α antibodies control inflammation in
Carolina Alves Nicolau et al.
Cellular immunology, 353, 104115-104115 (2020-05-11)
The CARMA1-BCL10-MALT1 (CBM) complex couples antigen receptors to the activation of Nuclear Factor κB (NF-κB) transcription factors in T/B lymphocytes. Within this signalosome, the MALT1 paracaspase serves dual roles: it is a crucial adaptor for signal transduction to NF-κB signaling
Jose A Guerrero-Martínez et al.
Nature communications, 11(1), 6196-6196 (2020-12-05)
The Transforming Growth Factor-β (TGFβ) signaling pathway controls transcription by regulating enhancer activity. How TGFβ-regulated enhancers are selected and what chromatin changes are associated with TGFβ-dependent enhancers regulation are still unclear. Here we report that TGFβ treatment triggers fast and
Constanza E Espada et al.
Journal of virology, 95(3) (2020-11-13)
Sterile alpha motif and HD domain-containing protein 1 (SAMHD1) restricts HIV-1 replication by limiting the intracellular deoxynucleoside triphosphate (dNTP) pool. SAMHD1 also suppresses the activation of NF-κB in response to viral infections and inflammatory stimuli. However, the mechanisms by which
Or Kalchiem-Dekel et al.
American journal of respiratory cell and molecular biology, 63(2), 185-197 (2020-04-28)
The primary function of APOE (apolipoprotein E) is to mediate the transport of cholesterol- and lipid-containing lipoprotein particles into cells by receptor-mediated endocytosis. APOE also has pro- and antiinflammatory effects, which are both context and concentration dependent. For example, Apoe-/-

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