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Merck
CN

PZ0234

Sigma-Aldrich

PF-543 盐酸盐

≥98% (HPLC)

别名:

PF-05144543 盐酸盐, (2R)-1-[[[4-[[3-甲基-5-[(苯磺酰基)甲基]苯氧基]甲基]苯基]甲基] -2-吡咯烷甲醇 盐酸盐, (R)-(1-(4-((3-甲基-5-(苯磺酰基甲基)苯氧基)甲基)苄基)吡咯烷-2-基)甲醇 盐酸盐

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About This Item

经验公式(希尔记法):
C27H31NO4S · HCl
分子量:
502.07
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

储存条件

desiccated

颜色

white to light brown

溶解性

H2O: 20 mg/mL, clear

储存温度

−20°C

SMILES字符串

[H]Cl.CC1=CC(OCC2=CC=C(CN3[C@@H](CO)CCC3)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1

InChI

1S/C27H31NO4S.ClH/c1-21-14-24(20-33(30,31)27-7-3-2-4-8-27)16-26(15-21)32-19-23-11-9-22(10-12-23)17-28-13-5-6-25(28)18-29;/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;1H/t25-;/m1./s1

InChI key

WNKWAZFYPZMDGJ-VQIWEWKSSA-N

生化/生理作用

PF-543可刺激微管相关蛋白轻链3(LC3)的颗粒积累。它还会诱导LC3-I向LC3-II的转化,并受到自噬抑制剂,渥曼青霉素、3-甲基腺嘌呤(3-MA)和巴氟霉素A1的抑制。在人的头颈部鳞状细胞癌(SCC)细胞中,PF-543盐酸盐可促进坏死、凋亡和自噬。
PF-543盐酸盐是一种全新的、细胞可渗透的、有效的、选择性的鞘氨醇激酶-1(SphK1)抑制剂。 PF-543可抑制SphK1,其Ki值为3.6 nM,其与鞘氨醇具有竞争性,对SphK1的选择性是SphK2同种型的100倍以上。PF-543可将内源性S1P的水平降低10倍,并与鞘氨醇的水平成比例地增加。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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分析证书(COA)

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Yuliya Fakhr et al.
International journal of molecular sciences, 23(7) (2022-04-13)
Preeclampsia (PE) involves inadequate placental function. This can occur due to elevated pro-inflammatory tumor necrosis factor-α (TNF-α). In other tissues, TNF-α signals via sphingosine kinase 1 (SphK1). SphK1 hinders syncytial formation. Whether this occurs downstream of TNF-α signaling is unclear.
Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells.
Hamada M. et al,
Cell death discovery, 3, 17047-17047 (2017)
Stephen J Blake et al.
Cell reports. Medicine, 2(12), 100464-100464 (2022-01-15)
Immune agonist antibodies (IAAs) are promising immunotherapies that target co-stimulatory receptors to induce potent anti-tumor immune responses, particularly when combined with checkpoint inhibitors. Unfortunately, their clinical translation is hampered by serious dose-limiting, immune-mediated toxicities, including high-grade and sometimes fatal liver
Gang Pei et al.
The EMBO journal, 40(13), e106272-e106272 (2021-05-05)
Cellular stress has been associated with inflammation, yet precise underlying mechanisms remain elusive. In this study, various unrelated stress inducers were employed to screen for sensors linking altered cellular homeostasis and inflammation. We identified the intracellular pattern recognition receptors NOD1/2

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