PROTAC SMARCA2/4-degrader-1 is a small molecule classified as a proteolysis-targeting chimera (PROTAC), designed to selectively degrade specific proteins within cells. This compound targets the SMARCA2 and SMARCA4 proteins, which are part of the SWI/SNF chromatin remodeling complex and are implicated in various cancers and other diseases. The mechanism of action involves the recruitment of an E3 ubiquitin ligase, leading to ubiquitination and subsequent proteasomal degradation of the target proteins. Characteristics of PROTACs like this one include their bifunctional nature, possessing both a ligand for the target protein and a ligand for the E3 ligase, which facilitates the formation of a ternary complex. This innovative approach allows for the selective modulation of protein levels, offering potential therapeutic advantages over traditional inhibitors. Additionally, the specificity and efficacy of PROTACs can vary based on their chemical structure and the cellular context, making ongoing research essential for optimizing their use in therapeutic applications.

PROTAC SMARCA2/4-degrader-1

2568273-68-5: PROTAC SMARCA2/4-degrader-1 is a small molecule classified as a proteolysis-targeting chimera (PROTAC), designed to selectively degrade specific proteins within cells. This compound targets the SMARCA2 and SMARCA4 proteins, which are part of the SWI/SNF chromatin remodeling complex and are implicated in various cancers and other diseases. The mechanism of action involves the recruitment of an E3 ubiquitin ligase, leading to ubiquitination and subsequent proteasomal degradation of the target proteins. Characteristics of PROTACs like this one include their bifunctional nature, possessing both a ligand for the target protein and a ligand for the E3 ligase, which facilitates the formation of a ternary complex. This innovative approach allows for the selective modulation of protein levels, offering potential therapeutic advantages over traditional inhibitors. Additionally, the specificity and efficacy of PROTACs can vary based on their chemical structure and the cellular context, making ongoing research essential for optimizing their use in therapeutic applications.

<p>Compound I-430, known as SMARCA2/4-degrader-1, is a PROTAC degrader targeting SMARCA2 and SMARCA4. In A549 cells, it achieves degradation of SMARCA2/4 proteins with DC50s values under 100 nM and demonstrates a maximal degradation rate (Dmax%) exceeding 90% after a 24-hour treatment.</p>

CAS 2568273-68-5

PROTAC SMARCA2/4-degrader-1

PROTAC SMARCA2/4-degrader-1

Ref: TM-T200697