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Merck
CN

PZ0234

PF-543 盐酸盐

≥98% (HPLC), sphingosine kinase-1 inhibitor, powder

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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关于此项目

经验公式（希尔记法）:
C27H31NO4S · HCl
化学文摘社编号:
1415562-82-1
分子量:
502.07
UNSPSC Code:
12352200
PubChem Substance ID:
329823785
NACRES:
NA.77
MDL number:
MFCD28411614

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产品名称

PF-543 盐酸盐, ≥98% (HPLC)

SMILES string

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

InChI key

WNKWAZFYPZMDGJ-VQIWEWKSSA-N

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

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to light brown

solubility

H2O: 20 mg/mL, clear

storage temp.

−20°C

Quality Level

100

相关类别

Biochem/physiol Actions

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。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000508998
0000508998
0000443370
0000443370
0000311407

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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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