GSK235
GSK235 is an orally active, selective and allosteric endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with pIC50 values of 8.45 and 7.59 for human and mouse ERAP1, respectively. GSK235 exhibits over 1000-fold selectivity for the two most homologous enzymes, ERAP2 and IRAP. GSK235 can regulate the immunopeptidome of cancer cells and enhance cancer cell antigenicity. GSK235 can be used for the study of colorectal cancer and arthritis[1].
Product Specifications
UNSPSC
12352005
Target
Aminopeptidase
Related Pathways
Metabolic Enzyme/Protease
Field of Research
Cancer; Inflammation/Immunology
Smiles
CC1=C(C#N)C(N2C[C@H](C(C)C)[C@@H](C(O)=O)C2)=NC(NC3(C)CCOCC3)=C1
Molecular Formula
C21H30N4O3
Molecular Weight
386.49
References & Citations
[1]Christopher P. Tinworth, et al. Discovery of an orally available potent ER aminopeptidase 1 (ERAP1) inhibitor that enhances anti-tumor responses and limits inflammatory autoimmunity in vivo. bioRxiv. November 17, 2025.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Curated Selection
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