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Merck
CN

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
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

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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