PROTACs, molecular glues and other degraders

SD-36 is a potent and efficacious STAT3 PROTAC degrader ( K d =~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (

SD-91.

SD-91.

SI-109 is a potent STAT3 SH2 domain inhibitor ( K i =9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 ( IC 50 =3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC

SIAIS164029.

SIAIS164029.

SIAIS178.

SIAIS178.

SIM1.

SIM1.

SJ988497.

SJ988497.