PF 543 hydrochloride (Synonyms: Sphingosine Kinase 1 Inhibitor II hydrochloride) |
| Catalog No.GC50253 |
PF 543 염산염(스핑고신 키나제 1 억제제 II 염산염)은 IC50이 2nM이고 Ki가 3.6nM인 강력하고 선택적이며 가역적이며 스핑고신 경쟁적인 SPHK1 억제제입니다.
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Cas No.: 1706522-79-3
Sample solution is provided at 25 µL, 10mM.
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
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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