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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: J Med Chem. 2015 Jan 8;58(1):183-96.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
Purity ≥98%
COA
MSDS
Compound 1 is a type II inhibitor. J Med Chem. 2015 Jan 8;58(1):183-96.
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.
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.