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.