567715
中性鞘磷脂酶抑制剂，GW4869
The N-SMase Inhibitor, GW4869, also referenced under CAS 6823-69-4, controls the biological activity of N-SMase. This small molecule/inhibitor is primarily used for Cell Signaling applications.
别名:
中性鞘磷脂酶抑制剂，GW4869, 中性神经鞘磷脂酶抑制剂GW4869，GW69A，GW554869A
InChI
1S/C30H28N6O2.2ClH/c37-27(35-25-11-7-23(8-12-25)29-31-17-18-32-29)15-5-21-1-2-22(4-3-21)6-16-28(38)36-26-13-9-24(10-14-26)30-33-19-20-34-30;;/h1-16H,17-20H2,(H,31,32)(H,33,34)(H,35,37)(H,36,38);2*1H/b15-5+,16-6+;;
InChI key
NSFKAZDTKIKLKT-CLEIDKRQSA-N
assay
≥90% (NMR)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
pale yellow
solubility
DMSO: 200 μg/mL
shipped in
wet ice
storage temp.
−20°C
Quality Level
General description
一种具有细胞渗透性的对称二氢咪唑酰胺化合物，可作为N-SMase（中性鞘磷脂酶）的有效、特异性、非竞争性抑制剂[IC50 = ~ 1 µM，大鼠脑；鞘磷脂的Km ~13 µM]。即使在150 µM下，也不抑制人类A-SMase（酸性鞘磷脂酶）。弱抑制牛蛋白磷酸酶2A和哺乳动物lyso PAF PLC的活性，而未观察到细菌磷脂酰胆碱特异性PLC的抑制。据报道，在20 µM时，可完全保护MCF7乳腺癌细胞中TNF-α或二胺诱导的细胞死亡护。不改变细胞内谷胱甘肽水平或干扰TNF-α或二胺介导的信号传递效应。
一种细胞可渗透的对称二氢咪唑酰胺，可作为中性鞘磷脂酶（N-SMase）的有效性、特异和非竞争性抑制剂（IC50 = 1 µM，大鼠脑N-SMase）。据报道，可在MCF7细胞中抑制肿瘤坏死因子α（TNF-α）诱导的鞘磷脂水解（20 µM时100%抑制）和TNF-α-诱导的细胞死亡。不干扰其他TNF-α-介导的信号事件，如从头神经酰胺合成、NF-κB激活和核转位。对通常因TNF-α而降低的细胞谷胱甘肽水平没有影响。不抑制酸性鞘磷脂酶（A-SMase）或细菌磷脂酰胆碱特异性磷脂酶C（PC-PLC）。显示弱抑制牛蛋白磷酸酶2A (PP2A)和人lyso PAF PLC，一种在体外水解鞘磷脂的酶。
Biochem/physiol Actions
主靶
N-Smase大鼠脑
N-Smase大鼠脑
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：1 µM大鼠脑N-SMase（中性鞘磷脂酶）；鞘磷脂的Km~13 µM
Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多3个月。
Other Notes
Marchesini, N., et al. 2003.J. Biol. Chem. In press.
Luberto, C., et al. 2002.J. Biol. Chem.277, 41128
Okamoto, Y., et al. 2002.FEBS Lett.530, 140.
Luberto, C., et al. 2002.J. Biol. Chem.277, 41128
Okamoto, Y., et al. 2002.FEBS Lett.530, 140.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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