HTH-01-015 |
Catalog No.GC13185 |
NUAK1 inhibitor,highly specific and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1613724-42-7
Sample solution is provided at 25 µL, 10mM.
HTH-01-015 is a highly specific inhibitor of NUAK1 with IC50 value of 100 nM 1.
HTH-01-015 showed extreme selectivity. It only inhibited the NUAK1 (NUAK family SNF1-like kinase-1) isoform of NUAK kinases and showed no significant inhibition of 139 other tested kinases. HTH-01-015 inhibited the phosphorylation of the NUAK1 substrate, MYPT1. The phosphorylated site was identified as Ser445. In HEK cells overexpressing drug-resistant NUAK1, HTH-01-015 displayed no more inhibition effect on MYPT1. In MEF cells, HTH-01-015 markedly reduced cell migration in the wound-healing assay. Besides that, HTH-01-015 impaired the proliferation at concentration of 10 μM both in U2OS cells and in MEF cells. Moreover, 10 μM HTH-01-015 also significantly inhibited the invasiveness of U2OS cells in a 3D matrigel transwell invasion assay 1.
References:
1. Sourav B, Sara J B, Hai-Tsang H, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochemical Journal, 2014, 457(1): 215-225.
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