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NEK7 degrader-3

SKU: orb3210796

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.

Images & Validation

Key Properties

CAS Number3119435-52-5
MW382.20
FormulaC16H13Cl2N3O4
SMILESO=C1NC(=O)C(C2=C(Cl)C=C(OC3(C4=NN=CO4)CC3)C=C2Cl)CC1
TargetInterleukin,MAPK,NOD-like Receptor (NLR),Molecular Glues,Caspase

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only
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Protocol Information