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HI-TOPK-032
🥰Excellent
Catalog No. T15481Cas No. 487020-03-1
HI-TOPK-032 is an effective and specific inhibitor of TOPK.
HI-TOPK-032
🥰Excellent
Purity: 98.52%
Catalog No. T15481Cas No. 487020-03-1
HI-TOPK-032 is an effective and specific inhibitor of TOPK.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $39 | In Stock | In Stock | |
| 5 mg | $63 | In Stock | In Stock | |
| 10 mg | $94 | In Stock | In Stock | |
| 25 mg | $198 | In Stock | In Stock | |
| 50 mg | $337 | In Stock | In Stock | |
| 100 mg | $579 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $68 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.52%
Appearance:Solid
Color:Orange
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | HI-TOPK-032 is an effective and specific inhibitor of TOPK. |
| In vitro | HI-TOPK-032 effectively suppresses both anchorage-dependent and independent growth of colon cancer cells by diminishing ERK-RSK phosphorylation and promoting apoptosis, evidenced by increased levels of p53, cleaved caspase-7, and cleaved PARP. At its highest concentration (5 μM), it also reduces MEK1 activity by 40%, showcasing its potency. While it significantly inhibits TOPK kinase activity, its impact on ERK1, c-jun-NH2-kinase 1, and p38 kinase activities remains minimal. The compound adeptly binds to the ATP-binding site of TOPK, forming hydrogen bonds with GLY83 and ASP151, and engaging in hydrophobic interactions with LYS30, highlighting its specificity and effective mechanism of action. |
| In vivo | HI-TOPK-032 (1 or 10 mg/kg; mice) treatment, obviously 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 caused, and phosphorylation of ERK and RSK, a direct downstream protein of ERK. Which is markedly inhibited in the HI-TOPK-032-treated group. |
| Molecular Weight | 369.4 |
| Formula | C20H11N5OS |
| Cas No. | 487020-03-1 |
| Smiles | O=C(Nc1ccn2c(c1)c(C#N)c1nc3ccccc3nc21)c1cccs1 |
| Relative Density. | 1.50 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 3.7 mg/mL (10.02 mM), Sonication is recommended.  | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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