Home >> Research Area >>Others>>SPHK>> PF-543 Citrate

PF-543 Citrate

SphK1 inhibitor,potent and cell-permeate CAS# 1415562-83-2

PF-543 Citrate

Catalog No. BCC1855----Order now to get a substantial discount!

Product Name & Size Price Stock
PF-543 Citrate:5mg $273.00 In stock
PF-543 Citrate:10mg $464.00 In stock
PF-543 Citrate:25mg $1092.00 In stock
PF-543 Citrate:50mg $1911.00 In stock
Molarity Calculator Dilution Calculator Send Mail Directly
Related Products

Quality Control of PF-543 Citrate

Quality Control & MSDS

Number of papers citing our products

Chemical structure

PF-543 Citrate

3D structure

Chemical Properties of PF-543 Citrate

Cas No. 1415562-83-2 SDF Download SDF
PubChem ID 71576669 Appearance Powder
Formula C33H39NO11S M.Wt 657.73
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (152.04 mM)
H2O : 50 mg/mL (76.02 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
Chemical Name [(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol;2-hydroxypropane-1,2,3-tricarboxylic acid
SMILES CC1=CC(=CC(=C1)OCC2=CC=C(C=C2)CN3CCCC3CO)CS(=O)(=O)C4=CC=CC=C4.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Standard InChIKey PWXXWUWKNPXSGW-VQIWEWKSSA-N
Standard InChI InChI=1S/C27H31NO4S.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/t25-;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PF-543 Citrate

DescriptionPF-543 Citrate is a novel cell-permeant inhibitor of SPHK1 with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.In Vitro:PF-543 is a novel selective sphingosine-competitive inhibitor of SphK1 that is over 1000-fold more potent in suppressing cellular S1P formation than DMS and SKI-2, commonly used pharmacological tools for SphK. PF-543 inhibits SphK1 with a Ki of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. In 1483 head and neck carcinoma cells, which are characterized by high levels of SphK1 expression and an unusually high rate of S1P production, PF-543 decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine[1]. PF-543 inhibits SphK1 in the in vitro enzyme assay with an IC50 value of 2.0±0.6 nM and is able to inhibit the enzyme >95% at a concentration of 20 nM[1]. PF-543 bounds in a bent conformation analogous to that expected of a bound sphingosine substrate but with a rotated head group[2].In Vivo:Administration of the potent sphingosine kinase 1 inhibitor, PF-543 in a mouse hypoxic model of pulmonary hypertension has no effect on vascular remodelling but reduces right ventricular hypertrophy. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[3].

References:
[1]. Schnute ME, 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. [2]. Wang J, et al. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33. [3]. MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55.

Protocol

Cell Assay [1]
1483, Jurkat andU937 cells are grown in 96-well plates in 100 μL of medium with PF-543 or DMSO vehicle (0.01%) at 37°C in an humidified incubator in the presence of 5% CO2. The cell growth and viability is measured using the CellTiter-Glo Assay by quantifying luminescence proportional to the amount of ATP present[1].

Animal Administration [3]
Mice: Two month old female mice (C57BL/6 J) are injected via the tail vein with RB-005 or PF-543 (10 or 30 mg/kg) dissolved in vehicle (PBS). 20 μL blood is withdrawn via tail vein bleeds at 15 min, 30 min, 1 h, 4 h, 6 h and 24 h following drug administration. Drug concentration is determined by MS analysis[3].

References:
[1]. Schnute ME, 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. [2]. Wang J, et al. Crystal Structure of Sphingosine Kinase 1 with PF-543. ACS Med Chem Lett. 2014 Oct 27;5(12):1329-33. [3]. MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55.

PF-543 Citrate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

PF-543 Citrate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of PF-543 Citrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5204 mL 7.6019 mL 15.2038 mL 30.4076 mL 38.0095 mL
5 mM 0.3041 mL 1.5204 mL 3.0408 mL 6.0815 mL 7.6019 mL
10 mM 0.152 mL 0.7602 mL 1.5204 mL 3.0408 mL 3.801 mL
50 mM 0.0304 mL 0.152 mL 0.3041 mL 0.6082 mL 0.7602 mL
100 mM 0.0152 mL 0.076 mL 0.152 mL 0.3041 mL 0.3801 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on PF-543 Citrate

PF-543 is a novel cell-permeant inhibitor of SphK1. PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 is the most potent inhibitor of SphK1 described to date and it will be useful for dissecting specific roles of SphK1-driven S1P signalling.

Featured Products
New Products
 

Description

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.

Keywords:

PF-543 Citrate,1415562-83-2,Natural Products,SPHK, buy PF-543 Citrate , PF-543 Citrate supplier , purchase PF-543 Citrate , PF-543 Citrate cost , PF-543 Citrate manufacturer , order PF-543 Citrate , high purity PF-543 Citrate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result:

      BioCrick BioTech
      88# Keyuan road,Hi-Tech Zone
      Chengdu, Sichuan 610042, PRC
      Email: info@biocrick.com
      Tel:86-28-8543-3893
      Follow us:

      BioCrick is one of the biggest natural products manufacturers in Asia

      Our products can be used as reference standards,inhibitors in pharmacological research

      Our MISSION is to provide Best-in-class High-purity natural compounds to researchers all around the world

      © 2007-2024 BioCrick BioTech. All rights reserved.  sitemap

      Menu Close
      Search Now