Art. -Nr.: HY-12334

HTH-01-015

1 Cited Publications

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HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC₅₀ is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).

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Reinheit: 99.10%
CAS. Nr.: 1613724-42-7
Formel: C₂₆H₂₈N₈O
Molecular Weight:468.55

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

HTH-01-015 Chemical Structure

CAS. Nr.: 1613724-42-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

HTH-01-015 is a selective NUAK1/ARK5 inhibitor (IC₅₀ is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).

IC₅₀ & Target^[1]

NUAK1

100 nM (IC₅₀)

Alle AMPK Isoform-spezifische Produkte anzeigen :

In Vitro

HTH-01-015 is a specific NUAK1 inhibitor. The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumor suppressor kinase. HTH-01-015 inhibits NUAK1 with an IC₅₀ of 100 nM, but does not significantly inhibit NUAK2 (IC₅₀ of >10 μM). In all cell lines tested, HTH-01-015 inhibits the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser⁴⁴⁵. In U2OS cells, HTH-01-015 suppresses proliferation and phosphorylation of MYPT1 to the same extent as shRNA-mediated NUAK1 knockdown. In mouse embryonic fibroblasts (MEFs), treatment with 10 μM HTH-01-015 suppresses proliferation and phosphorylation of MYPT1 to the same extent as NUAK1-knockout. To test whether NUAK1 inhibition impaired the ability of the invasive U2OS cells to enter a matrix, 3D Matrigel Transwell invasion assays demonstrate that 10 μM HTH-01-015 markedly inhibits the invasiveness of U2OS cells in this assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1613724-42-7
Appearance Solid
Molecular Weight 468.55
Formel C₂₆H₂₈N₈O
Color Light yellow to khaki
SMILES

O=C1C(C=C2C=CC=CC2=C3)=C3N(C)C4=NC(NC5=CN(N=C5)C6CCNCC6)=NC(C)=C4N1C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (1)

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Journal Impact Factor

J Cancer

LncRNA HOTAIR Enhances Epithelial-to-mesenchymal Transition to Promote the Migration and Invasion of Liver Cancer by Regulating NUAK1 via Epigenetic Inhibition miR-145-5p Expression. [Abstract]

2023 Jul 24;14(12):2329-2343. PMID: 37576402

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (213.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1342 mL

10.6712 mL

21.3424 mL

5 mM

0.4268 mL

2.1342 mL

4.2685 mL

10 mM

0.2134 mL

1.0671 mL

2.1342 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Kinase inhibitor specificity profiling assays are carried out against a panel of 140 protein kinases. Results are presented as a percentage of kinase activity in DMSO control reactions. Protein kinases are assayed in vitro with 0.1 or 1 μM of the inhibitors (e.g., HTH-01-015) and the results are presented as an average of triplicate reactions±S.D. or in the form of comparative histograms^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay kit. 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 or WZ4003. The ability of U2OS cells to invade in the presence or absence of 10 μM HTH-01-015 or WZ4003 is tested in a growth-factor-reduced Matrigel invasion chamber. Cells are serum-deprived for 2 h, detached using cell-dissociation buffer, and 2.5×10⁵ cells suspended in DMEM containing 1% (w/v) BSA are added to the upper chambers in triplicate and chemoattractant [DMEM containing 10% (v/v) FBS] is added to the lower wells. The chambers are kept at 37°C in 5% CO₂ for 16 h in the presence or absence of 10 μM HTH-01-015 or WZ4003 both in the upper and lower wells. Non-invaded cells are removed from the upper face of the filters by scraping, and cells that have migrated to the lower face of the filters are fixed and stained with Reastain Quick-Diff kit and images (×10 magnification) are captured. For cell invasion assays, statistical significance is assessed using GraphPad Prism 5.0^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Banerjee S, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1342 mL	10.6712 mL	21.3424 mL	53.3561 mL
	5 mM	0.4268 mL	2.1342 mL	4.2685 mL	10.6712 mL
	10 mM	0.2134 mL	1.0671 mL	2.1342 mL	5.3356 mL
	15 mM	0.1423 mL	0.7114 mL	1.4228 mL	3.5571 mL
	20 mM	0.1067 mL	0.5336 mL	1.0671 mL	2.6678 mL
	25 mM	0.0854 mL	0.4268 mL	0.8537 mL	2.1342 mL
	30 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7785 mL
	40 mM	0.0534 mL	0.2668 mL	0.5336 mL	1.3339 mL
	50 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0671 mL
	60 mM	0.0356 mL	0.1779 mL	0.3557 mL	0.8893 mL
	80 mM	0.0267 mL	0.1334 mL	0.2668 mL	0.6670 mL
	100 mM	0.0213 mL	0.1067 mL	0.2134 mL	0.5336 mL

Keywords

HTH-01-015

1 Cited Publications

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HTH-01-015

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Publications Citing Use of MedChemExpress (MCE) HTH-01-015

Alle AMPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HTH-01-015 Related Classifications

HY-12334 Related Classifications