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CAS No.: 1415562-82-1

PF-543 Catalog No. CSN17817

Synonyms: Sphingosine Kinase 1 Inhibitor II

PF-543 is a cell-permeant inhibitor of SphK1 with a Ki of 3.6 nM, PF-543 is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述PF-543 is a cell-permeant inhibitor of SphK1 with a Ki of 3.6 nM, PF-543 is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human PAMSC cells	100 nM	Function assay	24 h	Decrease of SK1 expression in human PAMSC cells at 100 nM after 24 hrs by Western blot analysis	24396570
Sf21 cells	-	Function assay	90 mins	Inhibition of His6 tagged human SphK1 expressed in Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins prior substrate addition by Caliper assay, Ki=4.3 nM	25516793
Sf9 cells	-	Function assay	-	Inhibition of human recombinant SphK1 expressed in Sf9 cells assessed as radiolabeled products using 5 uM sphingosine and 10 uM gamma[32P]ATP by liquid scintillation counting	25643074

参考文献

[1] Wang J, Knapp S, et al. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33.
[2] Schnute ME, McReynolds MD, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1478 mL
- 10.7388 mL
- 21.4777 mL
- 5 mM
- 0.4296 mL
- 2.1478 mL
- 4.2955 mL
- 10 mM
- 0.2148 mL
- 1.0739 mL
- 2.1478 mL

技术信息

CAS号	1415562-82-1	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C27H31NO4S	运输	蓝冰
分子量	465.60	别名	Sphingosine Kinase 1 Inhibitor II

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