Synonyms: compound 4 [Garnar-Wortzel et al., 2021]
Compound class:
Synthetic organic
Comment: SR-1114 is an ENL PROTAC degrader that was developed as part of the same study into ENL as an AML therapeutic target as the small molecule inhibitor SR-0813 [1]. Both SR-1114 and SR-0813 disrupt the transcriptional function of ENL. SR-1114 achieves this by directing ENL for cereblon-dependent degradation. SR-1114-induced ENL degradation is rapid, but reversible upon withdrawl of SR-1114, and leads to suppression of multiple ENL target genes (e.g. HOXA10, MYC, MYB, FLT3, ZEB2, and SATB1).
|
|
Bioactivity Comments |
The half-maximal degradation concentration (DC50) of SR-1114 vs. ENL in MV4;11 cells is 150 nM [1]. |