Basic information Safety Supplier Related

E3 ligase Ligand-Linker Conjugates 5 Free Base

Basic information Safety Supplier Related

E3 ligase Ligand-Linker Conjugates 5 Free Base Basic information

Product Name:
E3 ligase Ligand-Linker Conjugates 5 Free Base
Synonyms:
  • E3 ligase Ligand-Linker Conjugates 5 Free Base
  • (S,R,S)-AHPC-PEG3-NH2
  • VH032-PEG3-NH2
  • VHL Ligand-Linker Conjugates 1
  • PROTACs Related Compound 7
  • L-Prolinamide, N-[2-[2-[2-(2-aminoethoxy)ethoxy]ethoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-
  • (S,R,S)-AHPC-PEG3-NH2 (E3 ligase Ligand-Linker Conjugates 5)
  • (2S,4R)-1-((S)-14-amino-2-(tert-butyl)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS:
2010159-56-3
MF:
C30H45N5O7S
MW:
619.77
Mol File:
2010159-56-3.mol
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E3 ligase Ligand-Linker Conjugates 5 Free Base Chemical Properties

Boiling point:
879.2±65.0 °C(Predicted)
Density 
1.238±0.06 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
pka
13.54±0.46(Predicted)
form 
Solid
color 
Light yellow to yellow
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E3 ligase Ligand-Linker Conjugates 5 Free Base Usage And Synthesis

Description

(S, R, S)-AHPC-PEG3-amine hydrochloride salt is comprised of VHL Ligand coupled to an amine via a PEG3 linker. The 1 VHL Ligand 1 is a synthetic compound used in PROTAC research based on E3 ligase ligand. NH2 group is reactive with carboxylic acids in the presence of coupling reagent such as EDC , or directly with NHS esters, to form a stable amide bond.

Uses

(S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.

IC 50

VHL

References

[1] Chan KH, et al. Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds. J Me DOI:10.1021/acs.jmedchem.6b01912

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