PROTAC CB1R Degrader-1

PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547) ; Black: linker (HY-178198) ; Pink: CB1R ligand (HY-134497) ) [1].

Product Specifications

UNSPSC

12352005

Target

Akt; Apoptosis; Bcl-2 Family; Cannabinoid Receptor; ERK; PROTACs

Related Pathways

Apoptosis; GPCR/G Protein; MAPK/ERK Pathway; Neuronal Signaling; PI3K/Akt/mTOR; PROTAC; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

ClC(C=C1)=CC=C1C(N(N=C2C(NCCN3N=NC(CNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=C3)=O)C7=CC=C(C=C7Cl)Cl)=C2C

Molecular Formula

C35H28Cl3N9O5

Molecular Weight

761.01

References & Citations

[1]Kashkush A, et al. Development of PROTAC-Based Strategies for Cannabinoid Receptor Type 1 (CB1R) Degradation in Cancer. ACS Pharmacol Transl Sci. 2025 Sep 3;8 (9) :3160-3169.