SML2216
Takinib
≥98% (HPLC)
Synonym(s):
N1-(1-Propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide
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About This Item
Empirical Formula (Hill Notation):
C18H18N4O2
CAS Number:
Molecular Weight:
322.36
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
CCCN1C2=CC=CC=C2N/C1=N\C(C3=CC(C(N)=O)=CC=C3)=O
General description
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.
Biochem/physiol Actions
TAK-1 inhibitor
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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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
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
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