Synonyms: N-(4-Pyrrolidin-1-yl-piperidin-1-yl)-[4-(4-benzo[b]thiophen-2-yl-pyrimidin-2-ylamino)phenyl]carboxamide dihydrochloride; IKK16 hydrochloride
Molecular Formula: C28H29N5OS · 2HCl
Molecular Weight: 556.55
Linear Structural Formula: C28H29N5OS · 2HCl
Purity: >=98% (HPLC)
Storage: -20C
Application: IKK-16 dihydrochloride has been used as an nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor kinase inhibitor (I?B) in B220+ CKO or CreWT naive B cells. It has also been used as a nuclear factor kappa-light-chain-enhancer of activated B cells (NF-?B inhibitor) in poly(I:C) transfection-induced retinoic acid-inducible gene (RIG-I), melanoma differentiation-associated gene 5 (MDA-5), and caspase-11 expressing mouse embryonic fibroblasts (MEFs).
Biochem Physiol Actions: IKK-16 is a selective inhibitor of IKB kinase (IKK), part of the upstream NF-KB signal transduction cascade involved in the cellular response to inflammation. IKK-16 has IC50 values of 40, 70 and 200 nM for IKKbeta (IKK-2), IKK complex and IKKalpha (IKK-1) respectively. In a mouse sepsis model, IKK-16 reduced the multiple organ dysfunction, showing an antiinflammatory and endothelial protective effect likely mediated by inhibition of inflammation through NF-KB. IKK-16 has also been found to have some activity as an inhibitor of protein kinase D (PKD) and of multidrug resistance protein 1 (MDR1, ABCB1).