smarca2/4

Compound I-291, also known as PROTAC SMARCA2 4-degrader-30, targets the catalytic subunits of the SWI SNF complex, specifically SMARCA2 and SMARCA4. It effectively degrades SMARCA2 in A549 and MV411 cells, as well as SMARCA4 in MV411 cells, with a degradation concentration (DC50) of less than 100 nM.

SMARCA2 4-ligand-3, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis.

PROTAC SMARCA2 4-degrader-29 (Compound I-279) serves as a degrader for the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. In A549 cells, this compound effectively degrades SMARCA2 with a DC50 value of less than 100 nM, and similarly degrades SMARCA4 in MV411 cells with a DC50 under 100 nM.

PROTAC SMARCA2 4-degrader-25 is a PROTAC that targets SMARCA2 4. It consists of the E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, a PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid, and the target protein ligand SMARCA2 4-ligand-3. The conjugate of the E3 ubiquitin ligase ligand and Linker is (S,R,S)-AHPC.

PROTAC SMARCA2 4-degrader-28 (PROTAC 1) functions as a partial degrader of SMARCA2 and SMARCA4 through the PROTAC-based mechanism.

PROTAC SMARCA2 4-degrader-32 (compound I-446) is a PROTAC degrader targeting both SMARCA2 and SMARCA4 proteins. In A549 cells, it shows DC50s values for the degradation of SMARCA2 4 proteins <100 nM and achieves a maximum degradation rate (Dmax%) of >90 after 24 hours of treatment.

Compound I-431, also known as SMARCA2 4-degrader-2, is a PROTAC degrader targeting SMARCA2 and SMARCA4. In A549 cells, it degrades SMARCA2 4 proteins with DC50s values of less than 100 nM and achieves a maximum degradation rate (Dmax%) exceeding 90% after a 24-hour treatment.

Compound I-439, also known as SMARCA2 4-degrader-7, is a PROTAC degrader targeting SMARCA2 and SMARCA4. In A549 cells, it degrades SMARCA2 4 proteins with DC50s values less than 100 nM and achieves a maximum degradation rate (Dmax%) exceeding 90% after a 24-hour treatment.

SMARCA2 degrader-14 (compound I-408) is a PROTAC degrader targeting both SMARCA2 and SMARCA4. In A549 cells, it achieves degradation of SMARCA2 4 proteins with DC50s less than 100 nM and a maximal degradation rate (Dmax%) exceeding 90% after a 24-hour treatment.

PROTAC SMARCA2 4-degrader-33 (compound I-277) functions as a degrader targeting the proteins SMARCA2 and SMARCA4, exhibiting DC50s values of less than 100 nM for the degradation of SMARCA2 4 in A549 cells. After a treatment period of 24 hours, the maximum degradation rates (Dmax%) consistently exceed 90%.

SMARCA2 degrader-15 (compound I-409) is a PROTAC degrader targeting SMARCA2 and SMARCA4. In A549 cells, it achieves DC50s for SMARCA2 4 degradation of less than 100 nM, with a maximum degradation rate (Dmax%) exceeding 90% after a 24-hour treatment.

Compound I-430, known as SMARCA2 4-degrader-1, is a PROTAC degrader targeting SMARCA2 and SMARCA4. In A549 cells, it achieves degradation of SMARCA2 4 proteins with DC50s values under 100 nM and demonstrates a maximal degradation rate (Dmax%) exceeding 90% after a 24-hour treatment.

PROTAC SMARCA2 4-degrader-16 (compound I-337) serves as a PROTAC degrader targeting both SMARCA2 and SMARCA4 proteins, achieving DC50s values under 100 nM in A549 cells with a Dmax% exceeding 90 after 24 hours of treatment.

PROTAC SMARCA2 4-degrader-34 (compound 38) serves as an effective degrader of both SMARCA2 and SMARCA4. It demonstrates binding affinity to PXR with a DC50 value of 85.1 nM and reduces the protein expression of 3xFLAG-PXR.

PROTAC SMARCA2 4-degrader-35 (Ex.43) is a degrader of SMARCA2 4 with a DC50 value of less than 2.5 nM.

PROTACSMARCA2 4 degrader-36 (Compound 29) is a potent dual degrader targeting SMARCA2 and SMARCA4, exhibiting DC50 values of 0.22 nM and 0.85 nM, respectively. Additionally, PROTACSMARCA2 4 degrader-36 demonstrates antiproliferative activity.

SMARCA2 4-ligand-4 is a target protein ligand for PROTACs (Ligands for Target Protein for PROTACs). It is utilized in the synthesis of PROTAC SMARCA2 4 degrader-36.

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.

PROTAC SMARCA2 4-degrader-4 (Compound I-434) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. It efficiently degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM and degrades SMARCA4 in MV411 cells, also with a DC50 of less than 100 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.

PROTAC SMARCA2 4-degrader-5 (Compound I-437) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. It degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM and degrades SMARCA4 in MV411 with a DC50 ranging from 100 to 500 nM.

PROTAC SMARCA2 4-degrader-19 (Compound I-412) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. It degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM, and it degrades SMARCA4 in MV411 with a DC50 also under 100 nM.

SMARCA2 4-ligand-2 is a PROTAC target protein ligand.

PROTAC SMARCA2 4-degrader-9 (Compound I-503) is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI SNF complex. It effectively degrades SMARCA2 in MV411 and A549 cells, with a DC50 of less than 100 nM, and degrades SMARCA4 in MV411 with a similar DC50.