NEK7 degrader-3
NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation.
For research use only. We do not sell to patients.
- CAS No.: 3119435-52-5
- Formula: C16H13Cl2N3O4
- Molecular Weight:382.20
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Caspase Isoforms
More
Biological Activity
|
NEK7 33.1 nM (DC50) |
NLRP3 inflammasome |
Caspase-1 |
IL-1β |
IL-1α |
IL-18 |
NEK7 degrader-3 (Compound 322) (0.00001-10 μM) inhibits Caspase‑1 activity and suppresses the release of IL‑1β, IL‑1α and IL‑18 in human monocyte‑derived macrophages and microglia, and inhibits pyroptotic membrane permeabilization[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mice with LPS (HY-D1056)‑induced neuroinflammation[1]
-
Dosage:30 mg/kg
-
Administration:p.o.; bid for 5 days
-
Result:Induces NEK7 degradation and inhibited the production of IL‑1β and IL‑6 in brain tissues.
Chemical Information
-
CAS No. 3119435-52-5
-
Molecular Weight 382.20
-
Formula C16H13Cl2N3O4
-
SMILES
O=C1C(C2=C(Cl)C=C(OC3(CC3)C4=NN=CO4)C=C2Cl)CCC(N1)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz