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PZ0234

PF-543 盐酸盐

Name: PF-543 盐酸盐
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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属性

产品名称

PF-543 盐酸盐, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to light brown

solubility

H₂O: 20 mg/mL, clear

storage temp.

−20°C

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

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

说明

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

0000443370

0000311407

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Tumor Necrosis Factor-α Induces a Preeclamptic-like Phenotype in Placental Villi via Sphingosine Kinase 1 Activation.

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)

The immunotoxicity, but not anti-tumor efficacy, of anti-CD40 and anti-CD137 immunotherapies is dependent on the gut microbiota.

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

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