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).

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

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.

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.

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

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

IV-275 is a dual inhibitor targeting the bromodomains of both BRG1 and BRM. This compound not only augments DNA damage when combined with Temozolomide and Bleomycin but also suppresses the invasiveness of GBM cells. Furthermore, IV-275 amplifies Temozolomide-induced cell death and its apoptosis-inducing activity [1].

PROTAC BRM degrader-1 (compound 17) serves as a PROTAC-based degrader targeting both BRM and BRG1, exhibiting DC50 values of 93 pM and 4.9 nM, respectively [1].

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.

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.