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

HI-TOPK-032 

Cat. No.: HY-101550 Purity: 99.21%
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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10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
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10 mg USD 108 In-stock
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25 mg USD 234 In-stock
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50 mg USD 402 In-stock
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100 mg USD 696 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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].

Molecular Weight

369.40

Formula

C₂₀H₁₁N₅OS

CAS No.

487020-03-1

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 : ≥ 7.5 mg/mL (20.30 mM)

*"≥" means soluble, but saturation unknown.

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.
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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Keywords:

HI-TOPK-032TOPKT-LAK cell-originated protein kinaseInhibitorinhibitorinhibit

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