BiochemProbe — Life Science Research Reagents

VH032-NH2 free base · Synonyms: (S,R,S)-AHPC | VHL ligand 1

(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.

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

Research area Cancer
Purity >98% Stock Inquire

Description

(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.

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
CC1=C(SC=N1)C1=CC=C(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](N)C(C)(C)C)C=C1
InChIKey
ZLOXMSNKPDWMEF-ZIFCJYIRSA-N

Specifications

MW (average)
430.5640
Formula
C22H30N4O3S
CAS No.
1448297-52-6
Physical state
Solid
Color
White to light 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

References

[1]. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. Cancer Res. 2019 Jul 16. pii: canres.1236.2019.

Same research area

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