subunit

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 = 650 nM). It inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome, displaying low-nM to sub-nM IC50s. Thailanstatin A, as a payload for ADCs, is conjugated to the lysines on trastuzumab, yielding linker-less ADC.

PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader targeting the 20S proteasome subunit β5 (20Sproteasomesubunit β5), with a DC50 of 0.16 μM. It inhibits the proliferation of FaDu cancer cells, showcasing an IC50 of 0.23 μM. Additionally, PROTAC20Sproteasomesubunit β5 degrader 2 demonstrates antitumor activity in a mouse model.

PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) serves as a targeted degrader of the 20S proteasome subunit β5, exhibiting a DC50 value of 0.11 μM in FaDu cells. This compound disrupts the cell cycle and promotes apoptosis (apoptosis), while inhibiting cell proliferation and migration in both FaDu and KM3/BTZ cells. It is applicable for research into resistance to Bortezomib in pharyngeal carcinoma and multiple myeloma.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

PROTAC SMARCA2/4-degrader-8 (Compound I-502) is a PROTAC degrader targeting the catalytic subunit SMARCA of the SWI/SNF complex. It degrades SMARCA2 in A549 and MV411 cells with a DC50 of <100 nM and SMARCA4 in MV411 cells, also exhibiting a DC50 of <100 nM.

PROTACSMARCA2 degrader-5 (Compound I-425) functions as a PROTAC degrader targeting the catalytic subunit SMARCA2 of the SWI/SNF complex. It effectively degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM, and also degrades SMARCA4 in MV411, exhibiting a DC50 ranging from 100-500 nM.

PROTAC SMARCA2/4-degrader-20 (Compound I-405) is a PROTAC degrader targeting the catalytic subunit SMARCA2 in the SWI/SNF complex. It degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM. Additionally, it degrades SMARCA4 in MV411 with a DC50 ranging between 100 to 500 nM.