ML 9 a is myosin light chain kinase (MLCK) inhibitor. ML-9 enhances the anticancer activity of docetaxel, suggesting its potential application as an adjuvant to existing anticancer chemotherapy. The complex effect of ML-9 onautophagy and indentified ML-9 as an attractive tool for targetingautophagy in cancer therapy through dual inhibition of both theAkt pathway and the autophagy.
The Ca2+/calmodulin-dependent myosin light-chain kinase (MLCK) pathway is considered the primary regulatory pathway for contraction of airway smooth muscle. ML-9 is a membrane-permeable organic substance that has been identified as an inhibitor of MLCK. ML-9 at a concentration of 30 or 100μM inhibited Ca2+ mobilization induced by a high concentration of K+, methacholine, and thapsigargin in guinea pig tracheal smooth muscle.[2] ML-9 at 30μM reduced the phosphorylation of Akt in lymph node carcinoma of the prostate (LNCaP) cells. Treatment with ML-9 (1 – 50μM, 2 – 24h) also dose- and time-dependently increased the expression level of LC3-II in LNCaP cells. Treatment of LNCaP cells with 30μM ML-9 for 24h significantly induced prostate cancer cell death.[1]
作用机制
ML-9 is a membrane-permeable organic substance that has been identified as an inhibitor of MLCK, Akt kinase, and stromal interaction molecule 1.[1]
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