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IKK 16

CAS No. : 873225-46-8

MCE 国际站：IKK 16

产品活性：IKK 16 是一种选择性的 IκB 激酶 (IKK) 抑制剂，作用于 IKK2，IKK complex 和 IKK1，IC₅₀ 分别为 40 nM，70 nM 和 200 nM。IKK 16 还抑制富亮氨酸重复激酶 2 (LRRK 2)，IC₅₀ 为 50 nM。

研究领域：NF-κB  |  Autophagy

作用靶点：IKK  |  LRRK2

In Vitro: IKK 16 is a potent inhibitor of IKK2 with IC₅₀ value of 40 nM. 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%. 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.

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