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Merck
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주요 문서

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SML0789

Sigma-Aldrich

GI254023X

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

동의어(들):

(2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]-propyl]-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide, GI4023

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About This Item

실험식(Hill 표기법):
C21H33N3O4
CAS Number:
260264-93-5
Molecular Weight:
391.50
MDL number:
MFCD19381832
UNSPSC 코드:
12352200
PubChem Substance ID:
329825599
NACRES:
NA.77

product name

GI254023X, ≥98% (HPLC)

Quality Level

100

분석

≥98% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 15 mg/mL, clear

저장 온도

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

애플리케이션

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

생화학적/생리학적 작용

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

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문서 라이브러리 방문

ADAM10 cell surface expression but not activity is critical for Staphylococcus aureus α-hemolysin-mediated activation of the NLRP3 inflammasome in human monocytes.
Ezekwe E A D, et al.
Toxins, 8(4), 95-95 (2016)
The Mouse-specific Splice Variant mRAGE_v4 Encodes a Membrane-bound RAGE that is Resistant to Shedding and does not Contribute to the Production of Soluble RAGE.
Di Maggio S, et al.
PLoS ONE, 11(9), e0153832-e0153832 (2016)
Kazuhiro Aoki et al.
Developmental cell, 43(3), 305-317 (2017-11-08)
The biophysical framework of collective cell migration has been extensively investigated in recent years; however, it remains elusive how chemical inputs from neighboring cells are integrated to coordinate the collective movement. Here, we provide evidence that propagation waves of extracellular
Laura S Christian et al.
Cell reports, 35(6), 109118-109118 (2021-05-13)
As a critical machinery for rapid pathogen removal, resident memory T cells (TRMs) are locally generated after the initial encounter. However, their development accompanying tumorigenesis remains elusive. Using a murine breast cancer model, we show that TRMs develop in the tumor
Joshua A Kulas et al.
American journal of physiology. Endocrinology and metabolism, 316(1), E106-E120 (2018-11-14)
The amyloid precursor protein (APP) is a type I transmembrane glycoprotein widely studied for its role as the source of β-amyloid peptide, accumulation of which is causal in at least some cases of Alzheimer's disease (AD). APP is expressed ubiquitously
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