SML3768
EN67
≥98% (HPLC)
Synonym(s):
N-[[3-(3-Fluoro-4-methoxyphenyl)-4,5-dihydro-5-isoxazolyl]methyl]-2-propenamide, UBE2D recruiter EN67
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About This Item
Empirical Formula (Hill Notation):
C14H15FN2O3
CAS Number:
Molecular Weight:
278.28
NACRES:
NA.77
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell-permeable E2 UBE2D recruiter
EN67 is a cell-permeable, thiol-reactive acrylamido compound that preferentially and covalently binds E2 ubiquitin conjugating enzyme UBE2D family without affecting the enzymatic activity. EN67 is shown to selectively modify, yet reversibly, UBE2D2 allosteric cysteine-C111 without targeting the catalytic cysteine-C85. EN67 does not inhibit overall TP53 ubiquitination mediated by UBE2D2 and the whole ubiquitination machinery. PROTACs equipped with functionalized-EN67 warhead efficiently degrade the target proteins BRD4 and AR, respectively, in a UBE2D-dependent manner.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Targeted Protein Degradation through E2 Recruitment
ACS Chemical Biology, 18(4), 897-904 (2023)
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