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HTH-01-015

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Catalog No. T2374Cas No. 1613724-42-7

HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.

HTH-01-015

HTH-01-015

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Purity: 99.70%
Catalog No. T2374Cas No. 1613724-42-7
HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$37In StockIn Stock
2 mg$50In StockIn Stock
5 mg$72In StockIn Stock
10 mg$108In StockIn Stock
25 mg$223In StockIn Stock
50 mg$318In StockIn Stock
100 mg$428In StockIn Stock
1 mL x 10 mM (in DMSO)$79In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.70%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.
Targets&IC50
NUAK1:100 nM
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]
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.
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)
Chemical Properties
Molecular Weight468.55
FormulaC26H28N8O
Cas No.1613724-42-7
SmilesCN1c2cc3ccccc3cc2C(=O)N(C)c2c(C)nc(Nc3cnn(c3)C3CCNCC3)nc12
Relative Density.1.41 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 52 mg/mL (110.98 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 28 mg/mL (59.76 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.13 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.1342 mL10.6712 mL21.3424 mL106.7122 mL
5 mM0.4268 mL2.1342 mL4.2685 mL21.3424 mL
10 mM0.2134 mL1.0671 mL2.1342 mL10.6712 mL
20 mM0.1067 mL0.5336 mL1.0671 mL5.3356 mL
50 mM0.0427 mL0.2134 mL0.4268 mL2.1342 mL
DMSO
1mg5mg10mg50mg
100 mM0.0213 mL0.1067 mL0.2134 mL1.0671 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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