α-Synuclein

PROTACα-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with an EC50 of 1.57 μM and 4.09 μM, respectively. This compound plays a significant role in neurodegenerative disease (ND) research.

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 α-synuclein degrader 5 is a highly selective (PROTAC) compound targeting and degrading α-synuclein aggregates, with a DC50 value of 7.51 μM and a maximum degradation rate (Dmax) of 89%. It incorporates the probe molecule sery308 and E3 ligase ligands, suitable for neurological disease research [1].

Arg-PEG1-Tαsyn is a PROTAC degrader targeting α-synuclein (α-syn), with a DC50 of 0.28 μM in U251 cells. This compound utilizes arginine (Arg) as the E3 ligase ligand and a benzothiazole-aniline variant as the warhead for α-syn targeting. It effectively degrades both wild-type α-syn and its A53T mutant in mammalian cells. In vitro, Arg-PEG1-Tαsyn significantly reduces α-syn aggregation via the E3 ubiquitin ligase UBR1. In vivo, it demonstrates good safety and significantly improves dopaminergic neuron damage and motor dysfunction. Arg-PEG1-Tαsyn is useful in Parkinson's disease research.