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This category includes SMARCA2/SMARCA4 (BRM/BRG1) ATPase inhibitors and BRM/BRG1 ligands for laboratory research. SMARCA2 and SMARCA4 are alternative ATPase subunits of SWI/SNF chromatin remodeling complexes. The selection includes allosteric ATPase inhibitors and ligands listed as building blocks for degrader synthesis. Consult individual product records for target scope, compound properties and supporting references.
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 brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM.
FHT-2344 is a potent SMARCA4/SMARCA2 ATPase inhibitor with IC50 values of 0.026 μM for SMARCA4 and 0.013 μM for SMARCA2. It exhibits anticancer activity.
FHT-1204 is a potent inhibitor of SMARCA4 and SMARCA2 ATPases (BRG1 and BRM), with IC50 values of ≤10 nM for both targets.
FHT-1015 is a selective allosteric inhibitor of SMARCA4 (BRG1) and SMARCA2 (BRM), with IC₅₀ values of 4 nM and 5 nM, respectively. It binds to an allosteric site, inducing conformational changes that inhibit the ATPase activity of BRG1/BRM. FHT-1015 disrupts tumor cell growth and migration and is applicable in research on uveal melanoma and hematologic malignancies.
Synonyms: FHD-286
FHD-286 is a selective, orally active inhibitor of the SMARCA4/SMARCA2 (BRG1/BRM) ATPase. It holds potential for research into BAF (BRG1/BRM-associated factor)-related disorders, including acute myeloid leukemia.
BRM/BRG1 ATP Inhibitor-2 is a selective inhibitor of BRG1 and BRM ATPase activity, targeting the SWI/SNF chromatin remodeling complexes. This compound is valuable for investigating the molecular implications of BAF-related disorders, including cancer and developmental syndromes. Its mechanism of action enables researchers to explore the role of ATP-dependent chromatin remodeling in gene expression regulation and cellular differentiation.
BRM/BRG1 ATP Inhibitor-3 selectively targets the BRG1 and BRM ATPases, exhibiting inhibitory activity with IC50 values of 10.4 nM and 19.3 nM, respectively. This compound is valuable for investigating the roles of the BAF complex in various cancers and related disorders. Its effective inhibition of chromatin remodeling can provide insights into therapeutic strategies for targeting these pathways in oncology research.
BRM/BRG1 ATP Inhibitor-4 is a specific inhibitor targeting the BRG1 and BRM ATPases. This compound exhibits potent inhibition of the BAF complex, making it valuable for studying its role in oncogenesis and various disorders associated with chromatin remodeling. Research applications include investigating mechanisms of cancer progression and exploring therapeutic strategies for BAF complex-related diseases.
BRM/BRG1 ATP-IN-7 is a selective inhibitor targeting the SWI/SNF complexes BRM (SMARCA2) and BRG1 (SMARCA4), exhibiting IC50 values of 12 nM and 8 nM, respectively. This compound is valuable for investigating BRM/BRG1-dependent cancers, including non-small cell lung cancer and Ewing sarcoma, as well as certain virus-associated diseases, such as HPV infection. Its potent inhibition provides a useful tool for elucidating the roles of BRM and BRG1 in cancer biology and therapeutic development.
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BRM/BRG1 ATP-IN-5 is a potent inhibitor of the BRG1 and BRM proteins, targeting the BAF complex that plays a crucial role in ATP-dependent chromatin remodeling and gene expression regulation. This compound has demonstrated notable anti-tumor activity, particularly in cancers related to BAF complex dysfunctions. Its unique mechanism offers valuable insights for research into cancer biology and potential therapeutic approaches for BAF-associated malignancies.
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SMARCA2-IN-7 is a potent dual inhibitor of BRM and BRG1, demonstrating an IC50 of less than 0.005 µM for both targets. It exhibits significant anti-tumor activity, effectively inhibiting BRG1-deleted SKMEL5 tumor proliferation with an AAC50 of 13 nM. Additionally, it shows a cell proliferation activity AAC50 of 42 nM in H1299 cells. This compound serves as a valuable tool for researching the roles of BRM and BRG1 in cancer biology.
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BRM/BRG1 ATP-IN-8 is a selective inhibitor targeting the BRG1/BRM ATPase domain, demonstrating potent antitumor activity. By disrupting aberrant chromatin remodeling, this compound effectively induces apoptosis and growth arrest in cancer cells. BRM/BRG1 ATP-IN-8 is well-suited for research into BRG1/BRM-dependent malignancies, including hematological cancers, prostate cancer, breast cancer, and Ewing's sarcoma.
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SMARCA2-IN-10 is a selective inhibitor of the SMARCA2 ATPase domain, with an IC50 value of 17.676 μM. This compound has been shown to induce cell death in tumors lacking SMARCA4, making it a valuable tool for investigating SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma. Its targeting of the SMARCA2 ATPase offers significant potential for advancing research in these cancer types.
BRM/BRG1 ATP-IN-6 is a selective inhibitor targeting the BRG1/BRM components of the BAF complex, which plays a critical role in chromatin remodeling and gene expression through ATP dependency. This compound exhibits significant anti-tumor activity, particularly in cancers linked to dysregulation of the BAF complex. Its application in research provides insights into chromatin dynamics and potential therapeutic strategies for BAF complex-related malignancies.
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BRG1-IN-1 is a selective inhibitor of the SMARCA4/BRG1 complex, demonstrating enhanced efficacy in sensitizing glioblastoma (GBM) cells to the antiproliferative and cytotoxic effects of Temozolomide in vitro. This compound significantly enhances the therapeutic impact of Temozolomide on the growth of subcutaneous GBM tumors, making it a valuable tool for cancer research focused on overcoming drug resistance. Its application in investigating BRG1's role in tumor biology may provide insights into novel treatment strategies for GBM.
