HTH-01-015

Short Summary : NUAK1 inhibitor,highly specific and selective

Category : PI3K/Akt/mTOR Signaling|AMPK

Purity : 0.9808

CAS Number : 1613724-42-7

Formula : C26H28N8O

Molecular Weight :

Molecular Weight : 468.55

SMILE : CN1C(C2=CC3=CC=CC=C3C=C2N(C)C4=NC(NC5=CN(C6CCNCC6)N=C5)=NC(C)=C14)=O

Solubility : >23.5mg/mL in DMSO

Storage : Store at -20°C

Description : 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 M both in U2OS cells and in MEF cells. Moreover, 10 M 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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