Zomiradomide

Zomiradomide is an orally active PROTAC degrader for IRAK4 (DC50=6 nM), thereby inhibiting the NF-κB signaling pathway. Zomiradomide acts also as a molecular glue, recruiting Ikaros and Aiolos, and mediating their degradation (DC50 for Ikaros is 1 nM), thereby activating the type I IFN signaling pathway[1][2][3]. (Pink: target protein ligand PROTAC IRAK4 ligand-5 (HY-168311), Blue: E3 ligase ligand Thalidomide-4-Br (HY-W039116), Black: linker (HY-168313) )

Product Specifications

CAS Number

[2655656-99-6]

Product Name Alternative

KT-413

UNSPSC

12352005

Target

IFNAR; IRAK; NF-κB; PROTACs

Type

Reference compound

Related Pathways

Immunology/Inflammation; NF-κB; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/kt-413.html

Purity

95.43

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1C2C(NC(CC2)=O)=O)C3=CC=CC(NCCC(C4)CC4(C5)CN5C[C@H]6CC[C@H](C(SC7=C8)=NC7=CC(C(C)(O)C)=C8NC(C9=CC=CC(C(F)(F)F)=N9)=O)CC6)=C3C1=O

Molecular Formula

C45H48F3N7O6S

Molecular Weight

871.97

References & Citations

[1]Weiss Matthew M. Preparation of benzothiazole derivatives as IRAK degraders and uses thereof. World Intellectual Property Organization, WO2021127190 A1. 2021-06-24.|[2]Zeng S, et al. Current advances and development strategies of orally bioavailable PROTACs. Eur J Med Chem. 2023 Dec 5;261:115793.|[3]Weiss MM, et al., Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B-Cell Lymphoma. J Med Chem. 2024 Jul 11;67 (13) :10548-10566.