2007955-07-7
Chemical Structure
DG013A
- CAS. Nr.: 2007955-07-7
- Formula:C27H37N4O4P
- Molecular Weight:512.58
IUPAC Name: ((S)-2-(((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)carbamoyl)-4-methylpentyl)((R)-1-amino-3-phenylpropyl)phosphinic acid
InChIKey: QKFOTLXPIIESQI-IEZKXTBUSA-N
SMILES: O=P([C@@H](N)CCC1=CC=CC=C1)(O)C[C@@H](CC(C)C)C(N[C@H](C(N)=O)CC2=CNC3=CC=CC=C23)=O
Biological Activity: DG013A is a zinc-dependent M1-aminopeptidase inhibitor that exhibits inhibitory activity against ERAP1 (IC50 = 33 nM) and ERAP2 (IC50 = 11 nM). DG013A enhances SRHFLAFSFR epitope presentation, rescues GSW11 peptide neoantigen presentation, reduces SIINFEKL presentation, modulates the immunopeptidome, decreases HLA-B27 free heavy chain expression, and reduces IL-17A secretion. DG013A exhibits antiproliferative activity. DG013A can be used for research on autoimmune diseases and melanoma[1][2][3].
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DG013A | DG013A is a zinc-dependent M1-aminopeptidase inhibitor that exhibits inhibitory activity against ERAP1 (IC50 = 33 nM) and ERAP2 (IC50 = 11 nM). DG013A enhances SRHFLAFSFR epitope presentation, rescues GSW11 peptide neoantigen presentation, reduces SIINFEKL presentation, modulates the immunopeptidome, decreases HLA-B27 free heavy chain expression, and reduces IL-17A secretion. DG013A exhibits antiproliferative activity. DG013A can be used for research on autoimmune diseases and melanoma. | |||||||||||||||||||||
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References
- [1]. Wilding B, et al. Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1. Bioorganic & medicinal chemistry letters. 2021 Jun 15;42:128050. [Content Brief]
- [2]. Fougiaxis V, et al. ERAP Inhibitors in Autoimmunity and Immuno-Oncology: Medicinal Chemistry Insights. J Med Chem. 2024 Jul 25;67(14):11597-11621.
- [3]. Koumantou D, et al. Editing the immunopeptidome of melanoma cells using a potent inhibitor of endoplasmic reticulum aminopeptidase 1 (ERAP1). Cancer immunology, immunotherapy : CII. 2019 Aug;68(8):1245-1261.
