GI 254023X

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GI 254023X

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Cat No: 28284

Biochemicals - Small Molecule Inhibitors

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 ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(?R)-N-[(1S)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-?-[(1S)-1-(formylhydroxyamino)ethyl]-benzenepentanamide

Correlated keywords:

GI254023X GI254023-X 254023-X GI4023 SRI028594 ADAM-10 17 MMP1 MMP3 CX3CL-1 COS7 IL6 IL6R R interleukin THP1 LRP A?-42 40 HBMEC

Product Overview:
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.

Size	1 mg
Shipping	dry ice
CAS Number	260264-93-5
Molecular Formula	C₂₁H₃₃N₃O₄
SMILES	C[C@H](N(C=O)O)[C@H](C(N[C@@H](C(C)(C)C)C(NC)=O)=O)CCCC1=CC=CC=C1
Molecular Weight	391,5
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2921.29
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.