2-(2,6-dioxopiperidin-3-yl)-5-morpholinoisoindoline-1,3-dione

2-(2,6-dioxopiperidin-3-yl)-5-morpholinoisoindoline-1,3-dione Property

Boiling point:

643.7±55.0 °C(predicted)

Density 

1.460±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

solubility 

DMSO: Soluble: = 10 mg/ml

form 

Solid

pka

10.83±0.40(predicted)

color 

Light yellow to yellow

Hazard and Precautionary Statements (GHS)

2-(2,6-dioxopiperidin-3-yl)-5-morpholinoisoindoline-1,3-dione Chemical Properties,Usage,Production

Uses

PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms[1].

IC 50

Cereblon

References

[1] Mercer JAM, et al. Continuous evolution of compact protein degradation tags regulated by selective molecular glues. Science. 2024 Mar 15;383(6688):eadk4422. DOI:10.1126/science.adk4422