2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. HTH-01-015

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).

For research use only. We do not sell to patients.

HTH-01-015 Chemical Structure

HTH-01-015 Chemical Structure

CAS No. : 1613724-42-7

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 121 In-stock
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10 mg USD 154 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

HTH-01-015 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE HTH-01-015

View All AMPK Isoform Specific Products:

View All Isoforms
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

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.

HTH-01-015 Related Antibodies
Molecular Weight

468.55

Formula

C26H28N8O
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1342 mL 10.6712 mL 21.3424 mL
5 mM 0.4268 mL 2.1342 mL 4.2685 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
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].

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].

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

Complete Stock Solution Preparation Table

* 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.

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
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HTH-01-015 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HTH-01-0151613724-42-7AMPKAMP-activated protein kinaseInhibitorinhibitorinhibit

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