A TAK1 inhibitor
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Takinib

Item No. 24161

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-(1-propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide
CAS Number
1111556-37-6
Molecular Formula
C18H18N4O2
Formula Weight
322.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
323 nm
SMILES
O=C(C1=CC=CC(C(N)=O)=C1)NC2=NC3=CC=CC=C3N2CCC
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)
InChi Key
UOZVVPXKJGOFIG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $95

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    10 mg

    $169

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    25 mg

    $378

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    Product Description

    Takinib is a TGF-β-activated kinase 1 (TAK1) inhibitor (IC50 = 9.5 nM).1 It is selective for TAK1 over IRAK1, IRAK4, GCK, Clk2, and MINK1 (IC50s = 390, 120, 430, 430, and 1,900 nM, respectively). Takinib increases caspase-3/-7 activity and inhibits proliferation of TNF-α-stimulated, but not unstimulated, MDA-MB-231 cells in a concentration-dependent manner. It reduces phosphorylation of IKK, p38 MAPK, MAPK8, MAPK9, and c-Jun in TNF-α-stimulated MDA-MB-231 cells. Takinib inhibits IL-6 secretion in TNF-α-stimulated rheumatoid arthritis fibroblast-like synoviocytes in a concentration-dependent manner. It reduces inflammation and cartilage damage in knee joints in a mouse model of collagen type II-induced arthritis when administered at a dose of 50 mg/kg per day.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Totzke, J., Gurbani, D., Raphemot, R., et al. Takinib, a selective TAK1 inhibitor, broadens the therapeutic efficacy of TNF-α inhibition for cancer and autoimmune disease. Cell Chem. Biol. 24(8), 1029-1039 (2017).

    2. Scarneo, S.A., Eibschutz, L.S., Bendele, P.J., et al. Pharmacological inhibition of TAK1, with the selective inhibitor takinib, alleviates clinical manifestation of arthritis in CIA mice. Arthritis Res. Ther. 21(1), 292 (2019).