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

HI-TOPK-032 

Cat. No.: HY-101550 Purity: 98.83%
COA Handling Instructions

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

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 87 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 79 In-stock
Estimated Time of Arrival: December 31
10 mg USD 119 In-stock
Estimated Time of Arrival: December 31
25 mg USD 257 In-stock
Estimated Time of Arrival: December 31
50 mg USD 442 In-stock
Estimated Time of Arrival: December 31
100 mg USD 766 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE HI-TOPK-032

  • 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].

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

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

369.40

Appearance

Solid

Formula

C20H11N5OS
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (13.54 mM; Need ultrasonic)

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
10 mM 0.2707 mL 1.3535 mL 2.7071 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 0.5 mg/mL (1.35 mM); Clear solution

*All of the co-solvents are available by MCE.
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
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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.

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Keywords:

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

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