PF 543 hydrochloride

Name: PF 543 hydrochloride
Brand: Tocris Bioscience
SKU: 5754

Cat. No. 5754 2 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Discontinued Product

5754 has been discontinued.

View all Sphingosine Kinase products.

说明： Potent and selective SphK1 inhibitor

化学名： (2R)-1-[[(4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride

纯度： ≥98% (HPLC)

说明书

引用文献 (2)

生物活性技术数据说明书参考文献

生物活性 for PF 543 hydrochloride

PF 543 hydrochloride is a potent and selective SphK1 inhibitor (IC₅₀ = 2 nM; K_i = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P_1-5 receptors and 48 protein and lipid kinases. Inhibits growth and metastasis of several types of cancer cell including ovarian, colorectal and breast cancers, and suppresses HCT-116 tumor xenograft growth in mice. Antifibrotic and anti-inflammatory in a range of in vivo disease models. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.

许可信息

Sold for research purposes under agreement from Pfizer Inc.

化合物库 for PF 543 hydrochloride

PF 543 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for PF 543 hydrochloride

分子量	502.07
公式	C₂₇H₃₁NO₄S.HCl
储存	Desiccate at RT
纯度	≥98% (HPLC)
CAS Number	1706522-79-3
PubChem ID	121230770
InChI Key	WNKWAZFYPZMDGJ-VQIWEWKSSA-N
Smiles	CC1=CC(OCC2=CC=C(CN3CCC[C@@H]3CO)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1.Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

产品说明书 for PF 543 hydrochloride

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PF 543 hydrochloride

参考文献是支持产品生物活性的出版物。

Ju et al (2016) Targeting colorectal cancer cells by a novel sphingosine kinase 1 inhibitor PF-543. Biochem.Biophys.Res.Commun. 470 728 PMID: 26775841

Schnute et al (2012) Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem.J. 444 79 PMID: 22397330

Schnute et al (2017) Discovery of a potent and selective sphingosine kinase 1 inhibitor through the molecular combination of chemotype-distinct screening hits J.Med.Chem. 60 2562 PMID: 28231433

Zhang et al (2014) Elevated sphingosine-1-phosphate promotes sickling and sickle cell disease progression. J.Clin.Invest. 124 2750 PMID: 24837436

Yi et al (2023) Therapeutic potential of the sphingosine kinase 1 inhibitor, PF-543. Biomed.Pharmacother. 163 114401 PMID: 37167721

按标靶查看相关产品

按产品操作查看相关产品

查看全部 Sphingosine Kinase Inhibitors

关键词: PF 543 hydrochloride, PF 543 hydrochloride supplier, PF543, hydrochloride, potent, selective, sphingosine, kinase, kinases, Sphk1, inhibitors, inhibits, antifibrotic, fibrosis, inflammation, antiinflammatory, anticancer, metastasis, antimetastatic, breast, cancer, Sphingosine, Kinase, 5754, Tocris Bioscience

2 篇 PF 543 hydrochloride 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PF 543 hydrochloride 的部分引用包括：

Jiri et al (2021) A chemical screen for modulators of mRNA translation identifies a distinct mechanism of toxicity for sphingosine kinase inhibitors. PLoS Biol 19 e3001263 PMID: 34033645

Huilan et al (2021) aPC/PAR1 confers endothelial anti-apoptotic activity via a discrete, β-arrestin-2-mediated SphK1-S1PR1-Akt signaling axis. Proc Natl Acad Sci U S A 118 PMID: 34873055