化合物HTH-01-015 T2374

Product Introduction
Bioactivity


英文名: HTH-01-015

描述: HTH-01-015 是一种选择性 NUAK1 抑制剂，IC50为 100 nM。它抑制 NUAK1 的效力比抑制 NUAK2 高 100 倍以上，IC50大于10 μM。

细胞实验: 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)

激酶实验: 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.

体外活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4.69 mg/mL (10 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 28 mg/mL (59.8 mM)


关键字: inhibit | AMPK | AMP-activated protein kinase | HTH 01 015 | HTH01015 | Inhibitor | HTH-01-015

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相关库: AMPK-Targeted Compound Library | Anti-Liver Cancer Compound Library | Neuronal Differentiation Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Diabetic Compound Library | Highly Selective Inhibitor Library | Metabolism Compound Library | Glycolysis Compound Library

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