Acetamide, 2-chloro-N-(2-cyanoethyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-

Acetamide, 2-chloro-N-(2-cyanoethyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)- Property

Boiling point:

489.1±45.0 °C(Predicted)

Density 

1.351±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : 250 mg/mL (890.60 mM; Need ultrasonic)

pka

0.42±0.20(Predicted)

form 

Solid

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Acetamide, 2-chloro-N-(2-cyanoethyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)- Chemical Properties,Usage,Production

Uses

EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1[1].

Biological Activity

EN106 is a cell-permeable covalent recruiter of CUL2 E3 ligase FEM1B th at binds to C186 of FEM1B. EN106 disrupts FEM1B interactions with the FNIP1 degron and inhibits CUL2FEM1B-dependent ubiquitylation without detectable off-target effects. A modified EN106 bifunctional analog (PROTAC) recruits FEM1B and induces targeted BRD4 and BCR-ABL/c-ABL degradation.

References

[1] Henning NJ, et al. Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications. J Am Chem Soc. 2022;144(2):701-708. DOI:10.1021/jacs.1c03980