ERAP2-IN-1

• CAT Number: I043339
• CAS Number: 2420551-38-6
• Molecular Formula: C20H21F3N2O5S
• Molecular Weight: 458.45
• Purity: ≥95%
• Synonyms: 4-methoxy-3-[[2-piperidin-1-yl-4-(trifluoromethyl)phenyl]sulfamoyl]benzoic acid
• InChI: InChI=1S/C20H21F3N2O5S/c1-30-17-8-5-13(19(26)27)11-18(17)31(28,29)24-15-7-6-14(20(21,22)23)12-16(15)25-9-3-2-4-10-25/h5-8,11-12,24H,2-4,9-10H2,1H3,(H,26,27)
• InChIKey: BGLAMEXMBJAJBI-UHFFFAOYSA-N
• SMILES: COC1=C(C=C(C=C1)C(=O)O)S(=O)(=O)NC2=C(C=C(C=C2)C(F)(F)F)N3CCCCC3

ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC50 of 27 μM and model peptide hydrolysis with an IC50 of 44 μM[1].

Reference

[1]. Arya R, et al. Phenylsulfamoyl Benzoic Acid Inhibitor of ERAP2 with a Novel Mode of Inhibition. ACS Chem Biol. 2022 Jun 29.
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