2-アミノ-6-[2-(シクロヘキシルメトキシ)-6-ヒドロキシフェニル]-4-(4-ピペリジニル)-3-ピリジンカルボニトリル 化学特性,用途語,生産方法
酵素阻害剤
This novel IKK inhibitor (FW = 364.44 g/mol; CAS 406208-42-2; Soluble to 20 mM in DMSO), also named 2-amino-6-[2-(cyclopropylmethoxy)-6hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile, targets IκB kinases, with respective IC50 values of 8.5 and 250 nM for IKKβ and IKKα. ACHP’s selectivity is indicated by its > 20-μM IC50 values toward IKK3, Syk, and MAPKKK4. Inhibition of the TNFα-mediated gene expression could occur at low ACHP concentration (<1 μmol/L), with higher concentrations (>10 μmol/L) required to inhibit the constitutive phosphorylation of p65, expression of NF-κB-mediated genes (e.g., CYCLIN D1, BCL-xL, XIAP, c-IAP1, and IL-6), ultimately achieving myeloma cytostasis. Such findings indicate that ACHP’s growth inhibitory effects may be mediated through inhibition of both IKKα and IKKβ. By inhibiting NF-κB’s DNA binding activity, ACHP blocks the NF-κB pathway in multiple myeloma cell lines, inducing growth arrest and apoptosis.
2-アミノ-6-[2-(シクロヘキシルメトキシ)-6-ヒドロキシフェニル]-4-(4-ピペリジニル)-3-ピリジンカルボニトリル 上流と下流の製品情報
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