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PF 543

Product Name
PF 543
CAS No.
1415562-82-1
Chemical Name
PF 543
Synonyms
PF543;PF 543;CS-745;PF-543;PF543/PF-543;PF-543(freebase);PF 543 USP/EP/BP;Sphingosine Kinase 1 Inhibitor II;PF-543,anovelcell-permeantinhibitorofSPHK1;Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem
CBNumber
CB92645150
Molecular Formula
C27H31NO4S
Formula Weight
465.6
MOL File
1415562-82-1.mol
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PF 543 Property

storage temp. 
-20°C
solubility 
≥23.3 mg/mL in DMSO; insoluble in H2O; ≥51 mg/mL in EtOH with gentle warming and ultrasonic
form 
powder
color 
white to light brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0234
Product name
PF-543 hydrochloride
Purity
≥98% (HPLC)
Packaging
5MG
Price
$115
Updated
2023/01/07
Sigma-Aldrich
Product number
PZ0234
Product name
PF-543 hydrochloride
Purity
≥98% (HPLC)
Packaging
25MG
Price
$451
Updated
2023/01/07
Sigma-Aldrich
Product number
567741
Product name
Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem
Packaging
5mg
Price
$181
Updated
2023/01/07
Cayman Chemical
Product number
17034
Product name
PF-543
Purity
≥98%
Packaging
1mg
Price
$25
Updated
2021/12/16
Cayman Chemical
Product number
17034
Product name
PF-543
Purity
≥98%
Packaging
5mg
Price
$81
Updated
2021/12/16
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PF 543 Chemical Properties,Usage,Production

General Description

A cell-permeable hydroxymethylpyrrolidine compound that acts as a high affinity (Kd = 5 nM, kofft1/2 = 8.5 min), but poor, sphingosine kinase-1/SphK1 substrate (1/1,500 of sphingosine processivity) and potently inhibits against SphK1-catalyzed sphingosine-to-S1P conversion (IC50 = 2.0 nM; [sphingosine] = 3 μM) in a reversible, sphingosine-, but not ATP-, competitive manner (Ki = 3.6 nM), exhibiting 132-fold selectivity over SphK2, no affinity toward S1P receptors (S1P1, S1P2, S1P3, S1P5), and much reduced or no inhibitory activity against a panel of 46 other lipid and protein kinases (IC50 >10 μM), including the structurally related diacylglyerol kinase α/DAGKα (3.7% inhibition at 10 μM). PF-543 exposure in 1483 squamous cultures is reported to result in intracellular S1P depletion (by 90% upon 1 h 200 nM or 7 d 1 μM drug exposure) with concomitant elevation of sphingosine level and no detectable cytotoxicity (1 μM for 7 to 9 d in 1483, A549, Jurkat, LN229, MCF7, or U937 cultures). Also active in human whole blood assays in the presence human & bovine serum proteins (IC50 = 26.7 nM against cellular C17-S1P formation from exogenously added 20 μM C17-sphingosine in 10 min with 30 min drug preincubation).

Biological Activity

pf-543 is a novel and cell-permeant inhibitor of sphingosine kinase (sphk1) with ic50 value of 3.6 nm [1],sphk1 is a kinase that phosphorylates sphingosine to sphingosine-1-phosphate (sip). sphk1 is normally a cytosolic protein but can be recruited to the membrane to conduct its activity. it is the major source of production of s1p which promotes cell growth, survival and migration, and also regulate lymphocyte trafficking.biochemical study has identified that sphk1 was a sphingosine-competitive inhibitor but not atp-competitive [1]. in 1483 head and neck carcinoma cell cultures expressing high levels of sphk1 and with an unusually high rate of s1p production, pretreatment of pf-543 for 1 hr decreased the level of endogenous s1p by 10-fold with a proportional increase in the level of sphingosine. it indicated a significant inhibition of sphk1 by pf-543. however, specific inhibition of sphk1 had no effect on the proliferation and survival of 1483 cell cultures, despite a dramatic change in the cellular s1p/sphingosine rate [1].the inhibitory activity of pf-543 was also examined ex vivo in human whole blood. human whole blood with high sphk1 activity was prepared, which was able to quickly convert c17-sphingosine to c17-s1p. pf-543 treatment showed that pf-543 was a potent inhibitor of sphk1, capable of blocking >90% c17-s1p formation [1].

Biochem/physiol Actions

PF-543 hydrochloride is a novel, cell-permeable, potent and selective inhibitor of sphingosine kinase-1 (SphK1). 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. PF-543 decreased the level of endogenous S1P by 10-fold with proportional increase of the level of sphingosine.

References

[1] schnute m e et al. , modulation of cellular s1p levels with a novel, potent and specific inhibitor of sphingosine kinase-1. biochem j. 2012, 444(1): 79-88.

PF 543 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF 543 Suppliers

YouCoChem (Beijing) Chemical Technology Co., Ltd.
Tel
18800159827
Email
youcochem@163.com
Country
China
ProdList
132
Advantage
50
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2923
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
021-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6002
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-62063333-1 15601730970
Fax
021-50323701
Email
market@aladdin-e.com
Country
China
ProdList
24968
Advantage
65
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4863
Advantage
58
Shanghai Qinghang Chemical Co. Ltd.
Tel
021-50840321 / 18601625411
Fax
021-50840321
Email
thomasleehz@hotmail.com
Country
China
ProdList
216
Advantage
50
AdooQ Bioscience CHINA
Tel
025-58849295
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
3004
Advantage
60
Shanghai XR Chemical Technology Co., Ltd.
Tel
021-31007982 18019432809
Fax
021-31007982
Email
info@xrpharma.com
Country
China
ProdList
737
Advantage
55
Hubei Jusheng Technology Co.,Ltd
Tel
027-59599241 18871490274
Fax
027-59599241
Email
1400878000@qq.com
Country
China
ProdList
9824
Advantage
58
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View Lastest Price from PF 543 manufacturers

Career Henan Chemical Co
Product
PF 543 1415562-82-1
Price
US $2.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
100kg
Release date
2018-12-23

1415562-82-1, PF 543Related Search:


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