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PF 543

CAS No.
1415562-82-1
Chemical Name:
PF 543
Synonyms
PF543;CS-745;PF 543;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
Molecular Weight:
465.6
MDL Number:
MFCD23098794
MOL File:
1415562-82-1.mol
MSDS File:
SDS
Last updated:2023-05-18 11:30:59

PF 543 Properties

Boiling point 666.0±55.0 °C(Predicted)
Density 1.224±0.06 g/cm3(Predicted)
storage temp. -20°C
solubility ≥23.3 mg/mL in DMSO; insoluble in H2O; ≥51 mg/mL in EtOH with gentle warming and ultrasonic
pka 14.77±0.10(Predicted)
form powder
color white to light brown

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338

PF 543 price More Price(24)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 567741 Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem 1415562-82-1 5mg $187 2024-03-01 Buy
Sigma-Aldrich PZ0234 PF-543 hydrochloride ≥98% (HPLC) 1415562-82-1 5MG $115 2023-06-20 Buy
Sigma-Aldrich PZ0234 PF-543 hydrochloride ≥98% (HPLC) 1415562-82-1 25MG $451 2023-06-20 Buy
Cayman Chemical 17034 PF-543 ≥98% 1415562-82-1 1mg $25 2021-12-16 Buy
Cayman Chemical 17034 PF-543 ≥98% 1415562-82-1 5mg $81 2021-12-16 Buy
Product number Packaging Price Buy
567741 5mg $187 Buy
PZ0234 5MG $115 Buy
PZ0234 25MG $451 Buy
17034 1mg $25 Buy
17034 5mg $81 Buy

PF 543 Chemical Properties,Uses,Production

Definition

ChEBI: [(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]-2-pyrrolidinyl]methanol is a sulfonamide.

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.

target

SphK1

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

Global( 76)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29919 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6313 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 29831 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10523 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58
Nantong HI-FUTURE Biology Co., Ltd.
+undefined18051384581 sales@chemhifuture.com China 3136 58
TargetMol Chemicals Inc.
+1-781-999-5354 support@targetmol.com United States 19973 58
ShenZhen Trendseen Biological Technology Co.,Ltd.
13417589054 trendseenbio@gmail.com China 11681 58

View Lastest Price from PF 543 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
PF 543 pictures 2019-07-06 PF 543
1415562-82-1
US $2.00 / kg 1kg 99% 100kg Career Henan Chemical Co
  • PF 543 pictures
  • PF 543
    1415562-82-1
  • US $2.00 / kg
  • 99%
  • Career Henan Chemical Co

PF 543 Spectrum

PF 543 PF543 PF-543 PF543/PF-543 (2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)Methyl]phenoxy]Methyl]phenyl]Methyl]-2-pyrrolidineMethanol 2-PyrrolidineMethanol, 1-[[4-[[3-Methyl-5-[(phenylsulfonyl)Methyl]phenoxy]Methyl]phenyl]Methyl]-, (2R)- CS-745 PF-543(freebase) Sphingosine Kinase 1 Inhibitor II, PF-543 - CAS 1415562-82-1 - Calbiochem [(2R)-1-[[4-[[3-(benzenesulfonylmethyl)-5-methylphenoxy]methyl]phenyl]methyl]pyrrolidin-2-yl]methanol {1-[4-({3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy}methyl)benzyl]-2-pyrrolidinyl}methanol Sphingosine Kinase 1 Inhibitor II PF 543 USP/EP/BP PF-543,anovelcell-permeantinhibitorofSPHK1 1415562-82-1 Inhibitors