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PROTAC IRAK4 degrader-13

PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC50s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research[1]. Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker

Product Specifications

CAS Number

[2432992-21-5]

UNSPSC

12352005

Target

Interleukin Related; IRAK; PROTACs; Toll-like Receptor (TLR)

Related Pathways

Immunology/Inflammation; PROTAC

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

O=C(C1=NC(C(F)(F)F)=CC=C1)NC2=CC3=CN([C@H]4CC[C@H](CN(C5CCN(CC6=C(C(N7C(CC8)C(NC8=O)=O)=CC=C6)N(C)C7=O)CC5)C)CC4)N=C3C=C2C(C)(O)C

Molecular Formula

C44H52F3N9O5

Molecular Weight

843.94

References & Citations

[1]Veronica C, et al. Irak degraders and uses thereof. WO2021257914A1. 2021-12-23.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

IL-1; IL-17; IL-22; IL-23; IL-6; IL-8; IRAK4

Curated Selection

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