SML0789

GI254023X

≥98% (HPLC), powder, ADAM10 metalloproteinase inhibitor

• Synonym(s): (2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]-propyl]-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide, GI4023
• Empirical Formula (Hill Notation): C₂₁H₃₃N₃O₄
• CAS Number: 260264-93-5
• Molecular Weight: 391.50
• MDL number: MFCD19381832
• UNSPSC Code: 12352200
• PubChem Substance ID: 329825599
• NACRES: NA.77

Properties

• product name: GI254023X, ≥98% (HPLC)
• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 15 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: ON(C=O)[C@@H](C)[C@@H](CCCC1=CC=CC=C1)C(N[C@@H](C(C)(C)C)C(NC)=O)=O
• InChI: 1S/C21H33N3O4/c1-15(24(28)14-25)17(13-9-12-16-10-7-6-8-11-16)19(26)23-18(20(27)22-5)21(2,3)4/h6-8,10-11,14-15,17-18,28H,9,12-13H2,1-5H3,(H,22,27)(H,23,26)/t15-,17+,18+/m0/s1
• InChI key: GHVMTHKJUAOZJP-CGTJXYLNSA-N

Description

Application

GI254023X has been used to inhibit ADAM10 (ADAM metallopeptidase domain 10).

Biochem/physiol Actions

GI254023X blocks ADAM10 (ADAM metallopeptidase domain 10) activity and decreases human leukocyte antigen (HLA)-mediated cytotoxicity and cleavage of extracellular E-cadherin in epithelial and endothelial cells.

GI254023X is a potent and selective ADAM10 metalloproteinase inhibitor with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). In a study using recombinant TACE and ADAM10 ectodomain, the IC₅₀ for GI254023X was 5.3 nM for ADAM10 vs 541 nM for TACE.

GI254023X is a potent and selective ADAM10 metalloproteinase inhibitor.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable