| Name | HTH-01-015 |
| Description | HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM. |
| Cell Research | Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96? AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015.(Only for Reference) |
| Kinase Assay | Kinase activity assays: In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-32P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-32P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 h. |
| In vitro | In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. HTH-01-015 suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, HTH-01-015 inhibits cell proliferation in both cell lines. [1] HTH-01-015 inhibitors markedly restricted cells from entering into mitosis in U2OS cells. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.13 mM), Sonication is recommended.
DMSO : 4.69 mg/mL (10.01 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 28 mg/mL (59.76 mM), Sonication is recommended.
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| Keywords | NUAK2 | NUAK1 | Inhibitor | inhibit | HTH-01-015 | HTH01015 | HTH 01 015 | AMPK | AMP-activated protein kinase |
| Inhibitors Related | Sesamol | Adenosine monophosphate | Adenosine 5'-monophosphate monohydrate | Chromium(III) acetate | Methyl cinnamate | Metformin hydrochloride | D-Arabinopyranose | Tranexamic acid | Chitosan oligosaccharide | Isovaleric acid | Danthron | D-Arabinose |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Cancer Cell Differentiation Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Metabolism Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Liver Cancer Compound Library |
United States
