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Merck
CN

SML2839

Sigma-Aldrich

SR-318

≥98% (HPLC)

别名:

5-Amino-N-(4-((3-cyclohexylpropyl)carbamoyl)benzyl)-1-phenyl-1H-pyrazole-4-carboxamide, SR 318, SR318

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About This Item

经验公式(希尔记法):
C27H33N5O2
分子量:
459.58
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

NC1=C(C(NCC2=CC=C(C(NCCCC3CCCCC3)=O)C=C2)=O)C=NN1C4=CC=CC=C4

InChI

1S/C27H33N5O2/c28-25-24(19-31-32(25)23-11-5-2-6-12-23)27(34)30-18-21-13-15-22(16-14-21)26(33)29-17-7-10-20-8-3-1-4-9-20/h2,5-6,11-16,19-20H,1,3-4,7-10,17-18,28H2,(H,29,33)(H,30,34)

InChI key

HXNUFFCHRIWTRZ-UHFFFAOYSA-N

生化/生理作用

Potent and selective p38α/β type-II inhibitor.
SR-318 is a potent and selective type-II inhibitor that targets p38α/β in an inactive DFG-out conformation with good kinome selectivity (p38α/β IC50 = 5/39 nM by radiometric kinase assay). SR-318 selectively inhibits p38α/β by cell-based NanoBRET assay (IC50 = 3.7 nM/p38α, 10 nM/p38β, 0.91 μM/ZAK, ≥3 μM/DDR1, DDR2, KIT, MYLK4, RSK4) and effectively blocks LPS-induced TNF-α release in human whole blood (IC50 = 283 nM). SR-321 is an inactive structural analog and the recommended negative control compound.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Sandra Röhm et al.
Journal of medicinal chemistry, 62(23), 10757-10782 (2019-11-09)
p38 mitogen-activated protein kinases are key mediators of environmental stress response and are promising targets for treatment of inflammatory diseases and cancer. Numerous efforts have led to the discovery of several potent inhibitors; however, so far no highly selective type-II

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