MRT67307 hydrochloride 是IKKε和TBK-1的双重抑制剂,IC50分别为 160 和 19 nM。MRT67307 hydrochloride 还抑制ULK1和ULK2,IC50分别为 45 和 38 nM,并且阻断细胞自噬 (Autophagy)。
产品描述
MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC 50 s of 160 and 19 nM, respectively [1]. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC 50 s of 45 and 38 nM respectively, and blocks autophagy in cells [2].
体外活性
MRT67307 inhibits IKK and TBK1 with IC 50 values of 160 and 19 nM when assayed at 0.1 mM ATP in vitro, but did not inhibit IKKα or IKKβ even at 10 μM [1]. MRT67307 (2 μM) prevents the phosphorylation of IRF3 in bone-marrow-derived macrophages (BMDMs). MRT67307 (2 μM) dose not inhibit the activation of JNK or p38 MAPK by poly(I:C) [1]. MRT67307 (1 nM-10 μM) prevents the production of IFNβ in macrophages [1]. MRT67307 (10 μM) is sufficient to reduce phospho-ATG13 to control levels [2]. MRT67307 (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs) [2]. MRT67307 (5 μM; 4 h) eliminates TBK1/IKKε-induced CYLD phosphorylation in 293T cells [3]. Western Blot Analysis [3] Cell Line: 293T cells Concentration: 5 μM Incubation Time: 4 hours Result: Abrogated TBK1/IKKε-induced CYLD phosphorylation.
Cas No.
2095432-39-4
分子式
C26H37ClN6O2
分子量
501.06
别名
MRT67307 hydrochloride
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years