VHL ligand 2 hydrochloride ((S,R,S)-AHPC-Me hydrochloride) Datasheet | DC26119

VHL ligand 2 hydrochloride ((S,R,S)-AHPC-Me hydrochloride) — Datasheet

CAT. NO. DC26119

Parameter	Value
Chemical Name	VHL ligand 2 hydrochloride ((S,R,S)-AHPC-Me hydrochloride)
CAS No.	1948273-03-7
Synonyms	VHL ligand 2 hydrochloride
Formula	C23H33ClN4O3S
M.Wt	481.06
SMILES	Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)cc1.Cl
Purity	>98%
Storage	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Chemical identity references

Biological Activity

VHL ligand 2 hydrochloride is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.

In Vitro

E3 ligase Ligand 1 is a VHL E3 ligase-binding ligand[1]. E3 ligase Ligand 1 is used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC. ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition[2].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

Target

Ligand for E3 Ligase[1]

References & source

[1]. WO/2017/030814A1

[2]. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(26), 7124-7129

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.