Fig. 1 · Structure
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(S,R,S)-AHPC-Me dihydrochloride
Ligands for E3 Ligase
(S,R,S)-AHPC-Me dihydrochloride targets the von Hippel-Lindau (VHL) protein as a ligand for E3 ligase recruitment. This compound serves as a critical precursor for the synthesis of ARV-771, a PROTAC degrader that utilizes the VHL E3 ligase to facilitate the degradation of BET proteins. It has demonstrated potent activity in degrading BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM, highlighting its potential for therapeutic applications in cancer research.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Ligand / Binder |
| CAS Number | 2504950-56-3 |
| Applications | Ligands for E3 Ligase |
| Formula | C23H34Cl2N4O3S |
| Molecular Weight | 517.51 |
| Synonyms | VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride |
| 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 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.