PROTAC PD-1/PD-L1 degrader-1

PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner[1].

Product Specifications

CAS Number

[2447066-37-5]

UNSPSC

12352005

Target

PD-1/PD-L1; PROTACs

Type

Reference compound

Related Pathways

Immunology/Inflammation; PROTAC

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/protac-pd-1-pd-l1-degrader-1.html

Purity

99.52

Solubility

DMSO : 210 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCC(N4CCN(C(C5N(CC6=CC(Cl)=C(OCC7=CC=CC(C8=CC=C9OCCOC9=C8)=C7C)C=C6OCC%10=CC=CC(C#N)=C%10)CCCC5)=O)CC4)=O

Molecular Formula

C59H58ClN7O11

Molecular Weight

1076.59

References & Citations

[1]Cheng B, Ren Y, Cao H, Chen J. Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1. Eur J Med Chem. 2020;199:112377.