PF 543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 是一种有效的、选择性的、可逆的和鞘氨醇竞争性的 SPHK1 抑制剂，IC50 为 2 nM，Ki 为 3.6 nM。
货号:ajcx27216
CAS:1706522-79-3
分子式:C27H31NO4S.HCl
分子量：502.07
溶解度:DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Potent and selective SphK1 inhibitor (IC50 = 2 nM; Ki = 3.6 nM). Exhibits >100-fold selectivity for Sphk1 over Sphk2. Also exhibits >5,000 fold selectivity over S1P1-5 receptors and 48 protein and lipid kinases. Attenuates proliferation and induces necrosis in human colorectal cancer cells in vitro. Suppresses HCT-116 tumor xenograft growth in mice. Also reduces sickling, hemolysis and inflammation in a transgenic mouse model of sickle cell disease.

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