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E3 ligase Ligand 1

Cat. No. M9826

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E3 ligase Ligand 1 Structure
Synonym:

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

Size Price Availability Quantity
100mg USD 120  USD120 In stock
500mg USD 420  USD420 In stock
1g USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

E3 ligase Ligand 1 (VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me 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. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.

Chemical Information
Molecular Weight 481.05
Formula C23H33ClN4O3S
CAS Number 1948273-03-7
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Kanak Raina, et al. Proc Natl Acad Sci U S A. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Related Ligand for E3 Ligase Products
OICR-8268

OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can be used in the development of DCAF1-based PROTACs.

BC-1215

BC-1215 is a novel inhibitor of F-box protein 3 (Fbxo3) activity. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 relieves allodynia by preventing ubiquitination-dependent Fbxl2/TRAF2/TNIK/pGluR1 signaling. BC-1215 exerted robust therapeutic effects in cytokine-driven inflammation, including pseudomona-induced lung injury and cecum ligation/punctured-induced sepsis, by targeting Fbxo3/Fbxl2/TRAF-mediated cytokine release. BC-1215 can be used for the research of inflammation.

VH 101, acid 

VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development.

(S,R,S)-AHPC-Boc

(S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.

Lenalidomide-Br 

Lenalidomide-Br is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein.

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Keywords: E3 ligase Ligand 1, VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride supplier, Ligand for E3 Ligase, inhibitors, activators

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