LASSBio-1829 (hydrochloride)

LASSBio-1829 hydrochloride is an orally active IKK2 inhibitor with an IC₅₀ of 3.8 μM against the human target (Sf21 cells). LASSBio-1829 hydrochloride blocks signal transduction of the inflammation-associated NF-κB activation pathway. LASSBio-1829 hydrochloride reduces leukocyte migration, TNF-α biosynthesis, ROS production and NO production. LASSBio-1829 hydrochloride exhibits anti-inflammatory activity in a carrageenan-induced subcutaneous air pouch mouse model. LASSBio-1829 hydrochloride alleviates licking behavior during the inflammatory phase of the mouse formalin test. LASSBio-1829 hydrochloride can be used in inflammation-related research^[1]. In Vitro:LASSBio-1829 hydrochloride potently inhibits the human recombinant IKK2 enzyme expressed in Sf21 cells, with an IC₅₀ value of 3.8 μM^[1]. In Vivo:LASSBio-1829 (10-100 µM/kg; p.o.; single administration) hydrochloride exhibits potent oral anti-inflammatory activity in the carrageenan-induced subcutaneous air pouch mice model, and reduces leukocyte migration by up to 35%, TNF-α production by 46%, as well as ROS production in a dose-dependent manner^[1].
LASSBio-1829 (30 µM/kg; p.o.; single administration) hydrochloride alleviates inflammatory pain in mice in the formalin test, but shows no activity during the neuropathic pain phase^[1].