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

(S, R, S) -AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) 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 dihydrochloride 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

[2504950-56-3]

Product Name Alternative

VHL ligand 2 (dihydrochloride) ; E3 ligase Ligand 1 (dihydrochloride)

UNSPSC

12352005

Hazard Statement

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_dihydrochloride.html

Purity

99.84

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C) |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.Cl

Molecular Formula

C23H34Cl2N4O3S

Molecular Weight

517.51

Precautions

H315, H319, H335

References & Citations

[1]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.