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.

SMARCA2/4-ligand-5 is the target protein ligand of PROTAC SMARCA2/4 degrader-37 (Example 4). PROTAC SMARCA2/4 degrader-37 (Example 4) is a PROTAC degrader of SMARCA2/4, with an IC50 value of ≤0.1 μM.

PROTACSMARCA2/4 degrader-38 is a SMARCA2/4 PROTAC degrader with DC50 values of 3.0 nM and 4.0 nM, respectively. It facilitates the ubiquitination and degradation of SMARCA2/4 and can block the G0/G1 phase of the cell cycle, leading to the induction of apoptosis. PROTACSMARCA2/4 degrader-38 is applicable in acute myeloid leukemia (AML) research.

SMARCA2/4-ligand-6 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) utilized in the synthesis of SMARCA2/4-ligand-6.

SMARCA2/4 Ligand-Linker Conjugate 2 is a targeted protein ligand-linker conjugate that is used in the synthesis of [PROTAC] AU-15330.

SMARCA2/4 degrader-1 (Compound 1) is a molecular glue degrader specifically targeting SMARCA2/4, with a DC50 for SMARCA4 of 2.2 nM. It functions by covalently recruiting CUL4DCAF16 and CRL1FBXO22 to facilitate the degradation of SMARCA2/4.

BRM/BRG1 ligand 4 (Compound 6) is a SMARCA2/4 PROTAC degrader. It exhibits potent degradation activity against SMARCA2 and SMARCA4 in HeLa cells, with a DC50 of less than 0.1 nM. This compound is useful for researching cancers associated with abnormalities in SMARCA2/SMARCA4 or SWI/SNF mutations.

PROTACSMARCA2/4 degrader-39 (Compound 7) is a selective PROTAC degrader targeting SMARCA2 (BRM) and SMARCA4 (BRG1). This compound holds potential for research in oncology, including studies on non-small cell lung cancer and colorectal cancer.