MRT67307 hydrochloride 是IKKε和TBK-1的双抑制剂，IC50分别为 160 和 19 nM。MRT67307 hydrochloride 也可抑制ULK1和ULK2，IC50分别为 45 和 38 nM。MRT67307 hydrochloride 还抑制细胞自噬 (autophagy)。
| 生物活性 | MRT67307 hydrochloride is a dual inhibitor of theIKKεandTBK-1withIC50s of 160 and 19 nM, respectively[1]. MRT67307 hydrochloride also inhibitsULK1andULK2withIC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocksautophagyin cells[2]. |
| IC50& Target[1][2] | TBK1 19 nM (IC50, at 0.1 mM ATP) | IKKε 160 nM (IC50, at 0.1 mM ATP) | ULK2 38 nM (IC50) | ULK1 45 nM (IC50) | Autophagy |
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体外研究
(In Vitro) | MRT67307 inhibits IKKε and TBK1 with IC50values 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 suppresse 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) abrogates 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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