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    TAK1/MAP4K2 inhibitor 1
    TAK1/MAP4K2 inhibitor 1

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4589
    CAS #: 1315330-11-0Purity ≥98%

    Description: TAK1/MAP4K2 inhibitor 1 is a novel, potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively. It possesses good pharmacokinetic properties that will enable their use in pharmacological studies in vivo. A 2.4 Å cocrystal structure of TAK1 in complex with 1 confirms that the activation loop of TAK1 assumes the DFG-out conformation characteristic of type II inhibitors.

    References:  2015 Jan 8;58(1):183-96. 


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    TAK1/MAP4K2 inhibitor 1

    Molecular Weight: 552.59
    Formula: C₂₉H₃₁F₃N₆O₂
    CAS No.: 1315330-11-0
    SMILES: CC(N1)=CC2=C1N=CN=C2OC3=C(C)C=CC(C(NC4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4)=O)=C3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationTAK1/MAP4K2 inhibitor 1; TAK 1/MAP4K2 inhibitor 1; TAK-1/MAP4K2 inhibitor 1


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    These protocols are for reference only. InvivoChem does not independently validate these methods.

    TAK1/MAP4K2 inhibitor 1


    Compound 1 is a type II inhibitor. J Med Chem. 2015 Jan 8;58(1):183-96.

     TAK1/MAP4K2 inhibitor 1


    Evaluation of the ability of compounds to inhibit IL-1α, LPS, or CL097-induced phosphorylation of p105, p38, and JNK in several cell types. J Med Chem. 2015 Jan 8;58(1):183-96.

     TAK1/MAP4K2 inhibitor 1


    Evaluation of signaling following depletion of MAP4Ks by siRNA and evaluation of the ability of selective MAP4K2 inhibitors 16 and 17 to inhibit signaling in wild-type and TAK1-null MEF cells. J Med Chem. 2015 Jan 8;58(1):183-96.


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