gefitinib based protac 3

Gefitinib-based PROTAC 3, which connects an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) cells, respectively[1].

PROTAC MDM2 Degrader-3 utilizes PROTAC technology to degrade MDM2 by combining a potent MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.

PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.

PROTAC SOS1 Degrader-3 is a potent agent specifically designed to target and degrade SOS1 via the ubiquitin-proteasome system [1].

PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation mechanism of mutant EGFR [1].

PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau (VHL).

PROTAC FKBP Degrader-3 is a potent FKBP degrader, consisting of a FKBP ligand binding group, a linker, and a VHL binding group [1].

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.

PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein, reducing its levels by >80% at a concentration of 30 nM. Notably, this compound shows no activity against the ERRβ and ERRγ proteins.

PROTAC IRAK4 Ligand-3 serves as a ligand for PROTAC IRAK4 Degrader-7 and is utilized in cancer research [1].

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, used in cancer research.

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].

PROTAC α-synuclein degrader 3 (compound 5) is a potent and selective agent for degrading α-synuclein, used in Parkinson's disease research [1].

PROTAC BTK Degrader-3 is a potent degrader of Bruton's tyrosine kinase (BTK), with a DC50 (median degradation concentration) of 10.9 nM in Mino cells, and shows promise for research into B-cell malignancies, such as chronic lymphoid malignancies [1].