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Merck
모든 사진(1)

주요 문서

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SML2745

Sigma-Aldrich

GSK′481

≥98% (HPLC)

동의어(들):

(S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b]-[1,4]oxazepin-3-yl)isoxazole-3-carboxamide, GSK 2882481, GSK 481, GSK-2882481, GSK-481, GSK2882481, GSK481

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모든 사진(1)

About This Item

실험식(Hill 표기법):
C21H19N3O4
CAS Number:
1622849-58-4
Molecular Weight:
377.39
MDL number:
MFCD30343843
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

−20°C

SMILES string

N1(c2c(cccc2)OC[C@@H](C1=O)NC(=O)c3n[o]c(c3)Cc4ccccc4)C

InChI

1S/C21H19N3O4/c1-24-18-9-5-6-10-19(18)27-13-17(21(24)26)22-20(25)16-12-15(28-23-16)11-14-7-3-2-4-8-14/h2-10,12,17H,11,13H2,1H3,(H,22,25)/t17-/m0/s1

InChI key

KNOUWGGQMADIBV-KRWDZBQOSA-N

생화학적/생리학적 작용

A highly selective ATP site-targeting inhibitor against human/monkey, but not non-primate, RIP1.
GSK′481 is a highly potent receptor interacting protein 1 kinase (RIP1, RIPK1) inhibitor (human/monkey RIP1 IC50 = 1.6/2.5 nM; [ATP] = 50 μM) that targets RIP1 ATP-binding pocket with high affinity (kon = 0.66/μM/sec, t1/2 = 11 min) with little potency toward non-primate RIP1 (IC50 = 2.0/3.2/6.3/7.9/>10 μM against rabbit/mouse/rat/dog/minipig RIP1) and no off-target affinity when profiled at 10 μM by a 456-kinase panel. GSK′481 blocks caspase inhibitor/TNF-induced necroptosis in human monocytic U937 cultures (IC50 = 10 nM) and inhibits S166 autophosphorylation of exogenously expressed human, but not mouse, RIP1 in HEK293T transfectants (IC50 = 2.8 nM and >10 μM, respectively).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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시험 성적서(COA)

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문서 라이브러리 방문

Philip A Harris et al.
Journal of medicinal chemistry, 59(5), 2163-2178 (2016-02-09)
The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to its emergence as a highly promising target for the treatment of multiple inflammatory diseases. We screened RIP1 against
Shoko Nogusa et al.
Cell host & microbe, 20(1), 13-24 (2016-06-21)
Influenza A virus (IAV) is a lytic virus in primary cultures of many cell types and in vivo. We report that the kinase RIPK3 is essential for IAV-induced lysis of mammalian fibroblasts and lung epithelial cells. Replicating IAV drives assembly of

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