Revvity HTRF Total SMARCA-2 Detection Kit, 500 Assay Points

The SMARCA subgroup of genes belongs to the SWI/SNF family, involved in chromatin remodeling and DNA damage repair. SWI/SNF complexes regulate the genes involved in essential processes such as DNA replication, damage repair, and cell proliferation.

SMARCA4/BRG1 and SMARCA2/BRM are two mutually exclusive catalytic ATPase subunits of the SWI/SNF complex.

SMARCA4 loss of function is frequently associated with cancer, and a synthetic lethal relationship between SMARCA4 and SMARCA2 is well established in SMARCA4-deficient cancers, where the inactivation of SMARCA2 leads to tumor cell death.

Among therapeutic strategies being investigated to fight cancers, targeted protein degradation is expected to overcome some limitations from conventional small molecules. So far, PROTAC molecules have been developed to induce the selective degradation of SMARCA proteins. However, SMARCA2 and SMARCA4 share about 75% identity at the protein level, and so compounds are likely to target both proteins. Therefore, the selectivity of compounds targeting either SMARCA2 or SMARCA4 must be carefully investigated. In such investigations, the HTRF total SMARCA4 kit is a valuable companion assay for the HTRF total SMARCA2 kit, enabling reliable compound profiling.