Name: HTH-01-015
Price: 276.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    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.
    
    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.
- Properties
  - Alternative Name
    
    4,5,13-trimethyl-2-((1-(piperidin-4-yl)-1H-pyrazol-4-yl)amino)-5H-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6(13H)-one
    
    CAS Number
    
    1613724-42-7
    
    Molecular Formula
    
    C26H28N8O
    
    Molecular Weight
    
    468.55
    
    Appearance
    
    A solid
    
    Purity
    
    99.67%
    
    Solubility
    
    ≥23.45 mg/mL in DMSO; insoluble in H2O; ≥14.67 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

HTH-01-015

HTH-01-015

Background

We Also Recommend

p-Cresyl sulfate

Rucaparib (free base)

WWL 70