Art. -Nr.: HY-12334

HTH-01-015

Name: HTH-01-015
Brand: MedChemExpress
SKU: HY-12334
Price: 110.00 USD
Availability: InStock
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1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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

J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

Customer Validation & Images

Cell Migration/Invasion AssayWBRT-PCRIF

Cell Migration/Invasion Assay
WB
RT-PCR
IF
WB
Cell Migration/Invasion Assay

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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)

All Cell Migration/Invasion AssayWBRT-PCRIF

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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

HTH-01-015 purchased from MedChemExpress. Usage Cited in: J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

Added HTH-01-015 to SNU-387 and HepG2 cells, and Transwell test to detect cell invasion ability.

HTH-01-015 purchased from MedChemExpress. Usage Cited in: J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

Added HTH-01-015 to SNU-387 and HepG2 cells, and detected the protein expression of E-cadherin, N-cadherin, Vimentin, MMP2, MMP9 by Western blot.

HTH-01-015 purchased from MedChemExpress. Usage Cited in: J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

Added HTH-01-015 to SNU-387 and HepG2 cells, and detected the mRNA expression of E-cadherin, N-cadherin, Vimentin, MMP2, MMP9 by qPCR.

HTH-01-015 purchased from MedChemExpress. Usage Cited in: J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

Immunofluorescence of N-cadherin in cells treated with HTH-01-015 showed that the expression of N-cadherin protein was reduced compared with control cells.

HTH-01-015 purchased from MedChemExpress. Usage Cited in: J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

Transfected LZRS-HOTAIR plasmid in SNU-387 and HepG2 cells, and co-transfected LZRS-HOTAIR plasmid and HTH-01-015, used Western blot to detect the protein expression of E-cadherin, N-cadherin, Vimentin.

HTH-01-015 purchased from MedChemExpress. Usage Cited in: J Cancer. 2023 Jul 24;14(12):2329-2343. [Abstract]

To evaluate the role of NUAK1 in liver cancer invasion and migration, we next used HTH-01-015, an inhibitor of NUAK1, in transwell and scratch assays in SNU-387 and HepG2 cells. The results showed that inhibition of NUAK1 reduced the invasion and migration ability of liver cancer cells.

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

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

Bioz

Keywords

HTH-01-015

1 Cited Publications

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HTH-01-015

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

Alle AMPK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

In Vitro

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

In Vitro:

In Vivo:

In Vivo Dissolution Calculator

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HTH-01-015 Related Classifications

HY-12334 Related Classifications

Bioz

Keywords

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