brm/brg1

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

BRM/BRG1 ATP Inhibitor-2 is a BRG1/BRM ATPase inhibitor, suitable for studies on the treatment of BAF-related disorders.

PROTAC BRM/BRG1 degrader-4 (example 047) is a potent degrader targeting both BRM and BRG1, demonstrating DC50 values of 0.21 nM and 3.4 nM respectively in SW1573 cells.

PROTAC BRM/BRG1 degrader-2 (Example.004) is a potent PROTAC BRM/BRG1 degrading agent exhibiting a DC50 of less than 10 nM and an IC50 of 15 nM in A549 cells.

BRM/BRG1 ligand 3 is a target protein ligand utilized in the synthesis of PROTAC BRM/BRG1 degrader-3.

BRM/BRG1 Ligand 1 is a BRM/BRG1 ligand utilized for the synthesis of PROTAC BRM/BRG1 degrader-1.

PROTAC BRM/BRG1 degrader-1 is a chemical compound that acts as a degrader of PROTAC BRM/BRG1, exhibiting a DC50 range of 10-100 nM (BRM) and > 1 μM (BRG1). This compound is utilized in cancer research.

BRM/BRG1 ligand 2 serves as a target protein ligand for the synthesis of PROTAC BRM/BRG1 degrader-2.

PROTAC BRM/BRG1 degrader-3 (compound 304) is a PROTAC-based degrader of BRM/BRG1. In SW1573 cells, it degrades BRM with a DC50 of less than 1 nM and BRG1 with a DC50 greater than 1 nM. PROTAC BRM/BRG1 degrader-3 exhibits antitumor activity and inhibits the proliferation of A549 cells with an IC50 of 0.6 nM.

BRM/BRG1 ATP-IN-5 (Compound 6) is an inhibitor of BRG1/BRM. It targets the BAF complex, which plays a role in chromatin regulation and gene expression through ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-5 exhibits antitumor potential, particularly in cancers associated with disruptions in the BAF complex.

BRM/BRG1 ATP-IN-6 (Compound 105) is an inhibitor of BRG1/BRM. It acts on the BAF complex, which participates in chromatin regulation and gene expression through ATP-dependent chromatin remodeling. BRM/BRG1 ATP-IN-6 shows antitumor potential, particularly in cancers associated with BAF complex dysfunction.

BRM/BRG1 ATP-IN-7 (Compound Cpd69) functions as a selective dual inhibitor, effectively targeting BRM (SMARCA2) and BRG1 (SMARCA4) with IC50 values of 12 nM and 8 nM, respectively. It shows potential for research in BRM/BRG1-dependent cancers, such as non-small cell lung cancer and Ewing's sarcoma, as well as virus-associated diseases like HPV infection.

BRM/BRG1 ATP-IN-8 (Compound Cpd14) is an orally effective inhibitor of the BRG1/BRM enzyme domain. It exerts antitumor effects by disrupting aberrant chromatin remodeling in cancer cells, inducing apoptosis, and causing growth arrest. This compound is promising for research on BRG1/BRM-dependent malignancies, including hematologic cancers, prostate cancer, breast cancer, and Ewing's sarcoma.

BRM/BRG1 ATP degrader-1 (Compound 1) is a degrader of BRG1/BRM, with IC50 values of 0.01-0.1 μM for BRM IF degradation and greater than 0.1 μM for BRG1 IF degradation. This compound is applicable in cancer research studies.

BRM/BRG1 ATP Inhibitor-3 is a potent inhibitor targeting both BRM and BRG1 components of the BAF complex, with IC50 values of 10.4 nM for BRM and 19.3 nM for BRG1, and holds potential for research in cancer and BAF complex-related disorders.

BRM/BRG1 ATP Inhibitor-4, a potent inhibitor of BRG1/BRM, is utilized in the research of cancers and BAF complex-related disorders.

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

SMARCA2-IN-6 is a potent inhibitor of SMARCA2 (also known as BRM), exhibiting an IC50 of less than 5 nM against both SMARCA2 and SMARCA4. Additionally, this compound suppresses the expression of the KRT80 gene in H1299 cells with an IC50 of 26 nM and inhibits the proliferation of SKMEL5 cells carrying a BRG1 mutation with an IC50 value of 13 nM.

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1)/BRM/SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

E3 Ligase Ligand-linker Conjugate 126 is an E3 ligase ligand-linker conjugate designed for the synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-1.

PROTAC SMARCA2 degrader-29 (Example 87) is a potent PROTAC SMARCA2 (BRM) degrading agent with a DC50 ranging between 10-100 nM (BRM) and over 1 μM (BRG1, also known as SMARCA2).

trans-(S,R,S)-AHPC-Me-Amide-cyclohexane-pyrimidine-Cl is an E3 ligase ligand-Linker conjugate that is utilized in the synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-2.

E3 ligase Ligand 36 is an E3 ligase ligand that can be utilized for synthesizing PROTACs, such as PROTAC BRM/BRG1 degrader-1.

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.