Catalog No.: PC-72572Not For Human Use, Lab Use Only.
SR-1114 (SR1114) is a first-in-class ENL PROTAC degarder based on SR-0813 that binds to the E3 substrate adapter cereblon (CRBN), elicits rapid CRBN-dependent degradation of ENL with DC50 of 150 nM in MV4;11 cells.
SR-1114 (SR1114) is a first-in-class ENL degarder (PROTAC) based on SR-0813 that binds to the E3 substrate adapter cereblon (CRBN), elicits rapid CRBN-dependent degradation of ENL with DC50 of 150 nM in MV4;11 cells.
After withdrawal of SR-1114 from cells, ENL is rapidly resynthesized within 24 h.
ENL is also degraded by SR-1114 in MOLM-13 (DC50=311 nM) and OCI/AML-2 (DC50= 1.65 uM) cell lines.
SR-1114 treatment resulted in the preferential suppression of multiple ENL target genes, including HOXA10, MYC, MYB, FLT3, ZEB2, and SATB1, closely replicating the transcriptional consequences of dTAG-mediated ENL degradation.
The 16 h SR-1114 treatment (10 uM) also increased the abundance of the myeloid differentiation marker, CD11b, in agreement with the proposed role for ENL in preventing the terminal differentiation of AML cells.
