ACHP

ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC₅₀ values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies^[1][2][3][4]. IC50 & Target:IC50: 8.5 nM (IKK-β), 250 nM (IKK-α), >20000 nM (IKK3, Syk and MKK4)^[1] In Vitro:ACHP (0-100 µM; 3 days) inhibits cell growth with mean IC₅₀ of 26.8 µM in three myeloma cell lines (U266, NCUMM-2, ILKM-2)^[1].
ACHP (10 µM; 24 h) induces cycle arrest in U266 and NCUMM-2 cells^[1].
ACHP (10, 50 µM; 8 h) induces apoptosis in NCUMM-2 cells^[1].
ACHP (0-50 µM; 20 min) inhibits the phosphorylation of IkBa and p65 in MT-2 and ED-40515(-) cells^[2]. In Vivo:ACHP (0.3, 1, 3 mg/kg; p.o.; single) exhibits anti-inflammatory activity in Arachidonic acid-induced ear edema mice model^[3].