(brm)/smarca2

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

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

PROTAC SMARCA2 degrader-2, a selective and powerful degrader of SMARCA2/4, exhibits an IC50 of <0.1 μΜ in the HeLa HiBiT assay.this compound holds promise for research into cancers related to or deficient in SMARCA4 [1].

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).

SMARCA2-IN-7 (compound 12) acts as a dual inhibitor for both BRM and BRG1 with IC50 values less than 0.005, exhibiting antitumor proliferation effects. It inhibits tumor proliferation in SKMEL5 cells lacking BRG1 with an AAC50 of 13 nM. Additionally, in H1299 cells, it suppresses cell proliferation activity of KRT880 with an AAC50 of 42 nM.

SMARCA2-IN-8 (Compound 13) is an orally effective inhibitor targeting the SWI SNF chromatin remodeling complexes SMARCA2 (also known as Brahma homolog, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1), with IC50 values of 5 nM and 6 nM respectively. This compound inhibits the proliferation of SMARCA2-mutant SKMEL5 cancer cells with an AAC50 of 5 nM and downregulates the expression of the SMARCA2-dependent gene KRT80, showing an AAC50 of 10 nM. Additionally, SMARCA2-IN-8 demonstrates antitumor efficacy and favorable pharmacokinetic properties in mice.

FHT-1015 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with potential anticancer activity for the study of cancer and inflammation.

FHT-1204 is a potent inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) (IC50 ≤ 10 nM).