An ADAM10 inhibitor (IC50 = 5.3 nM); selective for ADAM10 over ADAM17

GI 254023X – 25 mg

Brand:
Cayman
CAS:
260264-93-5
Storage:
-20
UN-No:
Non-Hazardous - /

GI 254023X is an inhibitor of the metalloproteinase-disintegrin ADAM10 (IC50 = 5.3 nM).{50359} It is selective for ADAM10 over ADAM17, matrix metalloproteinase-1 (MMP-1), and MMP-3 (IC50s = 541, 108, and 187 nM, respectively), but also inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively). GI 254023X inhibits constitutive shedding of CX3CL1, but not shedding induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014), in COS-7 cells transfected with human chemokines (IC50s = 0.4 and >10 μM, respectively). It also inhibits constitutive, but not PMA-induced, secretion of the IL-6 receptor (IL-6R) from THP-1 macrophages (IC50s = 1.8 and >10 μM, respectively). GX 254023X (1 μM) decreases shedding of low density lipoprotein receptor-related protein 1 (LRP1) induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in human brain microvessel endothelial cells (HBMECs) and increases Aβ42 transit across an in vitro blood brain barrier model in a concentration-dependent manner.{50360} In vivo, GI 254023X (200 mg/kg) reduces brain LRP1 shedding and increases plasma levels of Aβ40 in a mouse model of Alzheimer’s disease.  

 

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Description

An ADAM10 inhibitor (IC50 = 5.3 nM); selective for ADAM10 over ADAM17, MMP-1 and MMP-3 (IC50s = 541, 108, and 187 nM, respectively); inhibits MMP-9 and MMP-13 (IC50s = 2.5 and 1.1 nM, respectively); inhibits constitutive, but not PMA-induced shedding of CX3CL1 in COS-7 cells transfected with human chemokines (IC50s = 0.4 and >10 μM, respectively); inhibits constitutive, but not PMA-induced, secretion of IL-6R from THP-1 macrophages (IC50s = 1.8 and >10 μM, respectively); decreases Aβ42-induced shedding of LRP1 in HBMECs; increases Aβ42 transit across an in vitro blood brain barrier model; reduces brain LRP1 shedding and increases plasma levels of Aβ40 in a mouse model of Alzheimer’s disease at 200 mg/kg

Formal name: (αR)-N-[(1S)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-α-[(1S)-1-(formylhydroxyamino)ethyl]-benzenepentanamide

Synonyms:  GI 4023|SRI 028594

Molecular weight: 391.5

CAS: 260264-93-5

Purity: ≥98%

Formulation: A crystalline solid

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