E3 ligase Ligand 1 free base · Synonyms: (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…

For research use only. Not for human or veterinary use.

Target Ligands for E3 Ligase

Research area Cancer

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Data Sheet SDS COA

E3 ligase Ligand 1 structure

CAS No.: 1948273-03-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 g	USD 800.00	BP-01952-25g	In stock	Get quote
50 g	USD 1,280.00	BP-01952-50g	In stock	Get quote
100 g	USD 2,050.00	BP-01952-100g	In stock	Get quote
500 g	Inquire	BP-01952-500g	In stock	Inquire

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Description

(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. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.

Biological activity

In Vitro The VHL protein is a substrate recognition subunit of two ubiquitously expressed and biologically important Cullin RING E3 ubiquitin ligase complexes. VHL is one of the most popular E3 ligases being recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and subsequent proteasomal degradation of a target protein.

Identifiers

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
InChIKey: GHFOLQCCYGBOTL-QDVBFIRISA-N

Specifications

MW (average): 481.0510
Formula: C₂₃H₃₃ClN₄O₃S
CAS No.: 1948273-03-7
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO and water

Documents

References

[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.

Same target

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