tcsc1282 IKK 16

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC₅₀s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC₅₀ of 50 nM.

IC50 & Target: IC50: 40 nM (IKK2), 70 nM (IKK complex), 200 nM (IKK1)^[1]


IC50: 50 nM (LRRK2)^[2]

In Vitro: IKK 16 is a potent inhibitor of IKK2 with IC₅₀ value of 40 nM^[1]. IKK 16, a leucine-rich repeat kinase-2 (LRRK2) kinase inhibitor, exhibits in vitro IC₅₀s of 50 nM. IKK 16 exhibits sub-micromolar IC₅₀ concentrations for LRRK2 in vitro, which is lower than what observed for cellular inhibition of Ser935 phosphorylation. IKK 16 (20 μM) can inhibit LRRK2 Ser935 phosphorylation in HEK293 GFP-LRRK2

G2019S cells (GS) or A2016T/G2019S (IRM) cells in vitro.

In Vivo: IKK 16 also demonstrates significant in vivo activity in an acute model of cytokine release. Both routes of administration of IKK 16 (30 mg/kg, sc) or orally (30 mg/kg, p.o) at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). IKK 16(10 mg/kg, sc) is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50%^[1]. Treatment of septic mice with IKK 16 (1 mg/kg body weight i.v.) results in a significantly increased degree of phosphorylation (P<0.05) of serine residues on Akt and eNOS in the liver^[3].