BMS-1166-N-piperidine-COOH

BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1[1]. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation[2].

Product Specifications

CAS Number

[2447066-00-2]

UNSPSC

12352005

Target

Ligands for Target Protein for PROTAC

Type

Reference compound

Related Pathways

PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bms-1166-n-piperidine-cooh.html

Purity

97.18

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1N(CCCC1)CC2=CC(Cl)=C(C=C2OCC3=CC=CC(C#N)=C3)OCC4=CC=CC(C5=CC=C6OCCOC6=C5)=C4C)O

Molecular Formula

C37H35ClN2O6

Molecular Weight

639.14

References & Citations

[1]Binbin Cheng, et al. Discovery of Novel Resorcinol Diphenyl Ether-Based PROTAC-like Molecules as Dual Inhibitors and Degraders of PD-L1. Eur J Med Chem. 2020 Aug 1;199:112377.|[2]Guzik K, et al. Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1. J Med Chem. 2017 Jul 13;60 (13) :5857-5867.