Takinib


Catalog No. size PriceQuantity
M7222-2 2mg solid $90
M7222-10 10mg solid $374

Description

Cas:1111556-37-6

Product Information

Takinib is a selective TAK1 inhibitor that induces apoptosis following TNF-α stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. 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.

 

Chemical Formula: C18H18N4O2

 

Exact Mass: 322.143

 

Molecular Weight: 322.36

 

Elemental Analysis: C, 67.07; H, 5.63; N, 17.38; O, 9.93

 

Synonym:

 

Takinib

EDHS-206

EDHS 206

EDHS206

 

Chemical Name:

3-N-(1-Propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide

 

InChi Key:

UOZVVPXKJGOFIG-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C18H18N4O2/c1-2-10-22-15-9-4-3-8-14(15)20-18(22)21-17(24)13-7-5-6-12(11-13)16(19)23/h3-9,11H,2,10H2,1H3,(H2,19,23)(H,20,21,24)

 

Smiles Code:

O=C(C1=CC=CC(C(NC2=NC3=CC=CC=C3N2CCC)=O)=C1)N

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

At 10 mM, Takinib shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1.

Analysis reveals that increasing concentrations of Takinib leads to a decrease in Vmax while maintaining KM. When the enzyme is activated with 5 mM ATP for 3 hr, the same Vmax is reached for 0, 10, 50, and 100 nM Takinib, and KM increases for these concentrations, which implies that Takinib is an ATP-competitive inhibitor if TAK1 is ATP activated. Importantly, results show that Takinib inhibits the function of both activated and un-activated TAK1 with identical potency.

TNF-α stimulation in the presence of Takinib induces caspase activity in MDA-MB-231 cells in a dose-dependent manner, whereas unstimulated cells do not upregulate caspase activity. 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 shows an almost complete inhibition of IL-6 secretion at micromolar concentrations following 24 hr of treatment in the presence of TNF-α.

 

 

References

 

  1. Totzke J, Gurbani D, Raphemot R, Hughes PF, Bodoor K, Carlson DA, Loiselle DR, Bera AK, Eibschutz LS, Perkins MM, Eubanks AL, Campbell PL, Fox DA, Westover KD, Haystead TAJ, Derbyshire ER. 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.e7. doi: 10.1016/j.chembiol.2017.07.011. PubMed PMID: 28820959; PubMed Central PMCID: PMC5576570.

 

Products are for research use only. Not for human use.

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