Reactivos e instrumentos para inmunología, biología celular y biología molecular.

PF-543 [1415562-82-1]

Imprimir

Referencia NB-64-31272-50mg

embalaje : 50mg

Marca : Neo Biotech

Solicitar más información

Remove All

PF-543

(Synonyms: Sphingosine Kinase 1 Inhibitor II, PF 543) Copy Product Info

Synonyms: Sphingosine Kinase 1 Inhibitor II, PF 543

Catalog No. T6085 Copy Product Info

Purity: 99.02%

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

Cas No. 1415562-82-1

For research use only—not for human use. No sales to individuals. Use as intended only.

Select Batch

Purity:99.02%

Appearance:Viscous

Color:Yellow

Product Introduction

Bioactivity

Description	PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.
Targets & IC50	SPHK1:2.0 nM, SPHK1:3.6 nM(Ki)
In vitro	PF543 is a cell-permeable hydroxyl methylpyrrolidine compound that inhibits SphK-1/SphK1-catalyzed sphingosine phosphorylation in a reversible and sphingosine-competitive manner, exhibiting no affinity toward S1P receptors and much reduced inhibitory activity against Sphk2 (6.8% inhibition at 10 μM) or 46 other lipid and portein kinases (IC50 >10 μM). In the SphK1-overexpression 1483 head and neck carcinoma cells, PF-543 decreases the level of endogenous S1P 10-fold with a proportional increase in the level of sphingosine. PF-543 binds SphK1 reversibly (k off t1/2=8.5 min) and with high affinity and the binding constant (Kd) is 5 nM. PF543 had no effect on the proliferation and survival of 1483, A549, LN229, Jurkat, U937 and MCF-7 cells, despite a dramatic change in the cellular S1P/sphingosine ratio. PF-543 is effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. [1]
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[2].
Synonyms	Sphingosine Kinase 1 Inhibitor II, PF 543
Kinase Assay	FITC-S1P quantification/Caliper assay: A 384-well format of the SphK enzyme assay based on separation of FITC-S1P from unreacted FITC-sphingosine substrate using a microfluidic capillary electrophoresis mobility-shift system is developed. Briefly, 3 nM SphK1–His6 is incubated with 1 μM FITC-sphingosine, 20 μM ATP and 10 μM compound (a final concentration of DMSO of 2 %) in a buffer containing 100 mM Hepes (pH 7.4), 1 mM MgCl2,0.01% Triton X-100, 10% glycerol, 100 μM sodium orthovanadate and 1 mM DTT for 1 h in a 384-well Matrical MP-101-1-PP plate. Reaction mixtures (10 μL) are quenched by the addition of 20 μL of 30 mM EDTA and 0.15% Coating Reagent-3 in 100 mM Hepes, and a small aliquot of each reaction (a few nanolitres) is analysed in the Caliper LabChip 3000 instrument under -1.5 psi (psi=6.9 kPa) pressure, a downstream voltage of -1900 V and a sip time of 0.2 s. Phosphorylated fluorescent product and unphosphorylated fluorescent substrate appeared as distinctive peaks and are quantified using the Caliper data.
Cell Research	CellTiter-Glo Assay (Only for Reference)

Chemical Properties

Molecular Weight	465.6
Formula	C₂₇H₃₁NO₄S
Cas No.	1415562-82-1
Smiles	Cc1cc(CS(=O)(=O)c2ccccc2)cc(OCc2ccc(CN3CCC[C@@H]3CO)cc2)c1
Relative Density.	1.224 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: <1 mg/mL

DMSO: 93 mg/mL (199.74 mM), Sonication is recommended.

Ethanol: 93 mg/mL (199.74 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 5 mg/mL (10.74 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.1478 mL	10.7388 mL	21.4777 mL	107.3883 mL
5 mM	0.4296 mL	2.1478 mL	4.2955 mL	21.4777 mL
10 mM	0.2148 mL	1.0739 mL	2.1478 mL	10.7388 mL
20 mM	0.1074 mL	0.5369 mL	1.0739 mL	5.3694 mL
50 mM	0.0430 mL	0.2148 mL	0.4296 mL	2.1478 mL
100 mM	0.0215 mL	0.1074 mL	0.2148 mL	1.0739 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

SphK1SphKsphingosine-competitiveSphingosine kinaseSK1S1PReceptorS1P ReceptorS1PPF-543PF543PAHNrf-2necrosisLysophospholipid ReceptorLPLReceptorLPL ReceptorLPLInhibitorinhibitcaspase-3/7AutophagyApoptosisanti-inflammatoryanti-cancer

Related Tags: PF-543 chemical structure | PF-543 in vivo | PF-543 in vitro | PF-543 formula | PF-543 molecular weight