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Merck
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주요 문서

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PZ0234

Sigma-Aldrich

PF-543 hydrochloride

≥98% (HPLC)

동의어(들):

(2R)-1-[[4-[[3-Methyl-5-[(phenylsulfonyl)methyl]phenoxy]methyl]phenyl]methyl]-2-pyrrolidinemethanol hydrochloride, (R)-(1-(4-((3-Methyl-5-(phenylsulfonylmethyl)phenoxy)methyl)benzyl)pyrrolidin-2-yl)methanol hydrochloride, PF-05144543 hydrochloride

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모든 사진(1)

About This Item

실험식(Hill 표기법):
C27H31NO4S · HCl
CAS Number:
1415562-82-1
Molecular Weight:
502.07
MDL number:
MFCD28411614
UNSPSC 코드:
12352200
PubChem Substance ID:
329823785
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

형태

powder

저장 조건

desiccated

색상

white to light brown

solubility

H2O: 20 mg/mL, clear

저장 온도

−20°C

SMILES string

[H]Cl.CC1=CC(OCC2=CC=C(CN3[C@@H](CO)CCC3)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1

InChI

1S/C27H31NO4S.ClH/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;/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3;1H/t25-;/m1./s1

InChI key

WNKWAZFYPZMDGJ-VQIWEWKSSA-N

생화학적/생리학적 작용

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.
PF-543 stimulates granular accumulation of microtubule-associated protein light chain 3 (LC3). It also induces LC3-I to LC3-II conversion, inhibited by autophagy inhibitors, wortmannin, 3-methyladenine (3-MA) and bafilomycin A1. In human head and neck squamous cell carcinoma (SCC) cells, PF-543 hydrochloride promotes necrosis,apoptosis and autophagy.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

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문서 라이브러리 방문

이미 열람한 고객

Slide 1 of 1

1 of 1

3-Methyladenine autophagy inhibitor

Sigma-Aldrich

M9281

3-Methyladenine

Yuliya Fakhr et al.
International journal of molecular sciences, 23(7) (2022-04-13)
Preeclampsia (PE) involves inadequate placental function. This can occur due to elevated pro-inflammatory tumor necrosis factor-α (TNF-α). In other tissues, TNF-α signals via sphingosine kinase 1 (SphK1). SphK1 hinders syncytial formation. Whether this occurs downstream of TNF-α signaling is unclear.
Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells.
Hamada M. et al,
Cell death discovery, 3, 17047-17047 (2017)
Gang Pei et al.
The EMBO journal, 40(13), e106272-e106272 (2021-05-05)
Cellular stress has been associated with inflammation, yet precise underlying mechanisms remain elusive. In this study, various unrelated stress inducers were employed to screen for sensors linking altered cellular homeostasis and inflammation. We identified the intracellular pattern recognition receptors NOD1/2

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