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Description: MS-444 is a novel, potent small-molecule inhibitor of HuR, which also inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 uM. MS-444 treatment of glioblastoma cells resulted in loss of viability and induction of apoptosis, with evidence implicating death receptor 5. BTICs were particularly sensitive to MS-444. At sub-lethal doses, MS-444 attenuated invasion of glioblastoma cells and BTICs in a transwell model. HuR is an RNA-binding protein implicated in immune homeostasis and various cancers, including colorectal cancer.
References: Lang M, Berry D, Passecker K, Mesteri I, Bhuju S, Ebner F, Sedlyarov V, Evstatiev R, Dammann K, Loy A, Kuzyk O, Kovarik P, Khare V, Beibel M, Roma G, Meisner-Kober N, Gasche C. HuR Small-Molecule Inhibitor Elicits Differential Effects in Adenomatosis Polyposis and Colorectal Carcinogenesis. Cancer Res. 2017 May 1; 77(9):2424-2438. doi: 10.1158/0008-5472.CAN-15-1726.
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