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Chemical Structure : SR-1114
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.
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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.
| M.Wt | 830.87 | |
| Formula | C39H42N8O11S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Garnar-Wortzel L, ACS Cent Sci. 2021 May 26;7(5):815-830.
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