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NEK7 degrader-3
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Catalog No. T218506 Copy Product Info
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NEK7degrader-3 is an orally active NEK7 molecular glue degrader capable of crossing the blood-brain barrier, with a DC50 of 31.1 nM. It facilitates the interaction between NEK7 and the E3 ligase cereblon, promoting NEK7 proteasomal degradation and reducing inflammation mediated by the NLRP3 inflammasome. NEK7degrader-3 inhibits caspase-1 activity, releases cytokines IL-1β, IL-1α, and IL-18, and decreases pyroptosis-related plasma membrane permeability. It shows anti-inflammatory effects in an LPS-induced neuroinflammation mouse model and is useful for studying neuroinflammation.
NEK7 degrader-3
Cas No. 3119435-52-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | NEK7degrader-3 is an orally active NEK7 molecular glue degrader capable of crossing the blood-brain barrier, with a DC50 of 31.1 nM. It facilitates the interaction between NEK7 and the E3 ligase cereblon, promoting NEK7 proteasomal degradation and reducing inflammation mediated by the NLRP3 inflammasome. NEK7degrader-3 inhibits caspase-1 activity, releases cytokines IL-1β, IL-1α, and IL-18, and decreases pyroptosis-related plasma membrane permeability. It shows anti-inflammatory effects in an LPS-induced neuroinflammation mouse model and is useful for studying neuroinflammation. |
| Targets & IC50 | NEK7:33.1 nM (DC50) |
| In vitro | NEK7 degrader-3 (Compound 322) (0.00001-10 μM) inhibits Caspase‑1 activity and prevents the release of IL‑1β, IL‑1α, and IL‑18 in macrophages derived from human monocytes and microglia, while also impeding pyroptotic membrane permeability. |
| In vivo | Compound 322, a NEK7 degrader, administered orally at 30 mg/kg twice daily for 5 consecutive days, facilitates the degradation of NEK7 and suppresses the production of IL-1β and IL-6 in the brain tissue of mice with LPS-induced neuroinflammation. |
| Molecular Weight | 382.20 |
| Formula | C16H13Cl2N3O4 |
| Cas No. | 3119435-52-5 |
| Smiles | O=C1NC(=O)C(C2=C(Cl)C=C(OC3(C4=NN=CO4)CC3)C=C2Cl)CC1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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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.
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Related Tags: NEK7 degrader-3 in vivo | NEK7 degrader-3 in vitro | NEK7 degrader-3 formula | NEK7 degrader-3 molecular weight
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