MRT 67307 dihydrochloride 是 IKKε 和 TBK-1 的双抑制剂,IC50 分别为 160 和 19 nM。MRT 67307 dihydrochloride 也可抑制 ULK1 和 ULK2,IC50 分别为 45 和 38 nM。MRT 67307 dihydrochloride 还抑制细胞Autophagy" style="display: inline; color: #c13a36">自噬 (Autophagy)。
产品描述
MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.
体外活性
MRT 67307 dihydrochloride inhibits IKKε and TBK1 with IC50 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]. MRT 67307 dihydrochloride (2 μM) prevents the phosphorylation of IRF3 in bone-marrow-derived macrophages (BMDMs). MRT 67307 dihydrochloride (2 μM) dose not suppresse the activation of JNK or p38 MAPK by poly(I:C)[1]. MRT 67307 dihydrochloride (1 nM-10 μM) prevents the production of IFNβ in macrophages[1]. MRT 67307 dihydrochloride (10 μM) is sufficient to reduce phospho-ATG13 to control levels[2]. MRT 67307 dihydrochloride (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs)[2]. MRT 67307 dihydrochloride (5 μM; 4 h) abrogates TBK1/IKKε-induced CYLD phosphorylation in 293T cells[3].
Cas No.
1781882-89-0
分子式
C26H38Cl2N6O2
分子量
537.53
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years