| 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. |
| Solubility Information | DMSO : 4.69 mg/mL (10 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 28 mg/mL (59.8 mM)
|
| Keywords | inhibit | AMPK | AMP-activated protein kinase | HTH 01 015 | HTH01015 | Inhibitor | HTH-01-015 |
| Inhibitors Related | Phenformin hydrochloride | AICAR | Doxorubicin hydrochloride | Adenosine monophosphate | ZLN024 | Metformin | Methyl cinnamate | A-769662 | Metformin hydrochloride | Chitosan oligosaccharide | Buformin hydrochloride | AMPK activator 4 |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Cancer Cell Differentiation Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Antioxidant Compound Library | Inhibitor Library | Mitochondria-Targeted Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
