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Cat. No.: HY-186342

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PROTAC NLRP3 degrader-1

PROTAC NLRP3 degrader-1 is a PROTAC degrader targeting NLRP3. PROTAC NLRP3 degrader-1 recruits VHL E3 ubiquitin ligase to form a ternary complex with NLRP3, inducing VHL-dependent ubiquitination and proteasomal degradation of the inflammasome sensor NLRP3. PROTAC NLRP3 degrader-1 reduces IL-1β release. PROTAC NLRP3 degrader-1 can be used for research on NLRP3-related inflammation, metabolic inflammation, and cancer.
(Pink: NLRP3 ligand (HY-186343); Blue: VHL ligand (HY-112078); Black: linker).

For research use only. We do not sell to patients.

CAS No.: 3115501-20-4
Formula: C₅₂H₆₇N₉O₈S₃
Molecular Weight:1042.34

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC NLRP3 degrader-1 Chemical Structure

CAS No.: 3115501-20-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

PROTAC NLRP3 degrader-1 is a PROTAC degrader targeting NLRP3. PROTAC NLRP3 degrader-1 recruits VHL E3 ubiquitin ligase to form a ternary complex with NLRP3, inducing VHL-dependent ubiquitination and proteasomal degradation of the inflammasome sensor NLRP3. PROTAC NLRP3 degrader-1 reduces IL-1β release. PROTAC NLRP3 degrader-1 can be used for research on NLRP3-related inflammation, metabolic inflammation, and cancer^[1]. (Pink: NLRP3 ligand (HY-186343); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target

^[1]

NLRP3

IL-1β

All PROTACs Isoforms :

All NOD-like Receptor (NLR) Isoforms :

All Interleukin Related Isoforms :

In Vitro

Innate ImmunityInflammasomeCytokines & Chemokines

Innate Immunity

Inflammasome

PROTAC NLRP3 degrader-1 (compound V2) simultaneously binds NLRP3 and VHL in vitro, increasing the thermal stability of NLRP3 and VHL in nanoDSF experiments^[1].
PROTAC NLRP3 degrader-1 (100-1000 nM) induces VHL-dependent, concentration-dependent NLRP3 degradation in THP-1 cells, reaching maximum degradation at 300 nM^[1].

Innate Immunity

Cytokines & Chemokines

Inflammasome

PROTAC NLRP3 degrader-1 (10 μM) inhibits IL-1β release in LPS (HY-D1056)-pretreated and Nigericin (HY-127019)-treated THP-1 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

CAS No. 3115501-20-4
Molecular Weight 1042.34
Formula C₅₂H₆₇N₉O₈S₃
SMILES

O=S(NC(NC1=C2C(CCC2)=CC3=C1CCC3)=O)(C4=CC(C(O)(C5=CN(N=N5)CCCCCCCC(N[C@@H](C(C)(C)C)C(N6[C@@H](C[C@H](C6)O)C(N[C@H](C7=CC=C(C8=C(N=CS8)C)C=C7)C)=O)=O)=O)C)=CS4)=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

Handling Instructions (2659 KB)

References

[1]. Keuler T, et al. Degrading the key component of the inflammasome: development of an NLRP3 PROTAC. Chemical communications (Cambridge, England). 2025 Feb 11;61(14):3001-3004.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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