(S, R, S) -AHPC-Me (hydrochloride)

(S, R, S) -AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S, R, S) -AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein[1]. (S, R, S) -AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 [2].

Product Specifications

CAS Number

[1948273-03-7]

Product Name Alternative

VHL ligand 2 (hydrochloride) ; E3 ligase Ligand 1

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Ligands for E3 Ligase

Type

Reference compound

Related Pathways

PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/E3_ligase_Ligand_1.html

Purity

99.95

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O.Cl

Molecular Formula

C23H33ClN4O3S

Molecular Weight

481.05

Precautions

H302, H315, H319, H335

References & Citations

[1]WO/2017/030814A1|[2]Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113 (26) :7124-9.