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Merck
CN

SML0789

GI254023X

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

别名:

(2R)-N-\ [(1S)-2,2-二甲基-1-\ [(甲氨基)羰基]-丙基]-2-\ [(1S)-1-\ [甲酰(羟基)氨基] 乙基]-5-苯基戊酰胺, GI4023

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关于此项目

经验公式(希尔记法):
C21H33N3O4
化学文摘社编号:
分子量:
391.50
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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产品名称

GI254023X, ≥98% (HPLC)

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 15 mg/mL, clear

storage temp.

2-8°C

Quality Level

Application

GI254023X 已被用于抑制 ADAM10(ADAM 金属肽酶结构域 10)。

Biochem/physiol Actions

GI254023X 是一种强效、选择性 ADAM10 金属蛋白酶抑制剂,对 α-分泌酶 ADAM10 的选择性是 ADAM17 (TACE) 的 100 倍。在使用重组 TACE 和 ADAM10 胞外域的研究中,GI254023X 的 IC50 ADAM10 为 5.3 nM,TACE 为 541 nM。
GI254023X 是一种强效选择性 ADAM10 金属蛋白酶抑制剂。
GI254023X 阻断 ADAM10(ADAM 金属肽酶域 10)的活性,并降低上皮细胞和内皮细胞中人类白细胞抗原 (HLA) 介导的细胞毒性和细胞外 E-cadherin 的裂解。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Ezekwe E A D, et al.
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Kazuhiro Aoki et al.
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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
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)
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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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