2. Cell Cycle/DNA Damage
  3. TOPK
  4. HI-TOPK-032

HI-TOPK-032 is a potent and specific TOPK inhibitor.

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

HI-TOPK-032 Chemical Structure

HI-TOPK-032 Chemical Structure

CAS No. : 487020-03-1

Size Price Stock Quantity
5 mg USD 79 In-stock
10 mg USD 119 In-stock
25 mg USD 257 In-stock
50 mg USD 442 In-stock
100 mg USD 766 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

HI-TOPK-032 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

HI-TOPK-032 is a potent and specific TOPK inhibitor.

In Vitro

HI-TOPK-032 strongly suppresses TOPK kinase activity but has little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. HI-TOPK-032 occupies the ATP-binding site of TOPK and fits the binding site very well. The compound forms hydrogen bonds with GLY83 and ASP151 and has a hydrophobic interaction with LYS30. However, HI-TOPK-032 at the highest concentration (5 μM) also inhibits MEK1 activity by 40%. HI-TOPK-032 also inhibits anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP[1].

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

HI-TOPK-032 Related Antibodies
In Vivo

Treatment of mice with 1 or 10 mg/kg of HI-TOPK-032 significantly inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well tolerated with HI-TOPK-032 treatment. The expression of p53 is strongly induced, and phosphorylation of ERK and RSK, a direct downstream protein of ERK, is markedly inhibited in the HI-TOPK-032-treated group[1].

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

369.40

Formula

C20H11N5OS
CAS No.
Appearance

Solid

Color

Pink to red

SMILES

O=C(C1=CC=CS1)NC2=CC3=C(C#N)C4=NC5=CC=CC=C5N=C4N3C=C2
Shipping

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

DMSO : 2.5 mg/mL (6.77 mM; ultrasonic and warming and heat to 60°C; 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 2.7071 mL 13.5355 mL 27.0709 mL
5 mM 0.5414 mL 2.7071 mL 5.4142 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: 0.25 mg/mL (0.68 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.5 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  15% Cremophor EL    85% Saline

    Solubility: 10 mg/mL (27.07 mM); Suspended solution; Need ultrasonic

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]

The effect of HI-TOPK-032 on ERK1, JNK1, and p38 activity is assessed by an in vitro kinase assay using ERK1 (active, 500 ng), inactive RSK2 (ERK1 substrate, 1 μg), JNK1 (active, 50 ng), c-Jun (JNK1 substrate, 1 μg) and p38 (active, 200 ng), and ATF2 (p38 substrate, 500 ng) with [γ-32P]ATP. Briefly, the reaction is carried out in the presence of 10 μCi of [γ-32P]ATP with HI-TOPK-032 (0.5, 1, 2, 5 μM) in 40 μL of reaction buffer. After incubation at room temperature for 30 minutes, the reaction is stopped by adding 10 μL protein loading buffer and the mixture is separated by SDS-PAGE[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

HCT-116 colon cancer cells are treated with different doses of HI-TOPK-032 (1, 2, 5 μM). After incubation for 1, 2, or 3 days, 20 μL of CellTiter96 AQueous One Solution is added and then cells are incubated for 1 hour at 37°C in a 5% CO2 incubator. Absorbance is measured at 492 nm[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Mice are divided into 4 groups: (i) untreated vehicle group; (ii) 1 mg HI-TOPK-032/kg of body weight; (iii) 10 mg HI-TOPK-032/kg of body weight; and (iv) no cells and 10 mg HI-TOPK-032/kg of body weight. HCT-116 cells are suspended in serum-free McCoy 5A medium and inoculated s.c. into the right flank of each mouse. HI-TOPK-032 or vehicle is injected 3 times per week for 25 days. Tumor volume is calculated[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7071 mL 13.5355 mL 27.0709 mL 67.6773 mL
5 mM 0.5414 mL 2.7071 mL 5.4142 mL 13.5355 mL
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HI-TOPK-032 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:

HI-TOPK-032487020-03-1TOPKT-LAK cell-originated protein kinaseInhibitorinhibitorinhibit

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