E3 ligase Ligand-Linker Conjugates 9 Property

Boiling point:

963.4±65.0 °C(Predicted)

Density 

1.195±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

Ethanol: 100 mg/mL (120.85 mM); DMSO: ≥ 100 mg/mL (120.85 mM)

pka

13.54±0.46(Predicted)

form 

Oil

color 

Light yellow to yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

E3 ligase Ligand-Linker Conjugates 9 Chemical Properties,Usage,Production

Uses

Protein degrader builiding block (S,R,S)-AHPC-PEG₆-Butyl chloride enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel–Lindau (VHL)-recruiting ligand, a linker with both hydrophobic and hydrophilic moieties, and a pendant chloroalkane for reactivity with a nucleophilic group on a target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant chloro group, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

reaction suitability

reactivity: sulfuryl reactive
reagent type: ligand-linker conjugate