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PF-543 (Synonyms: Sphingosine Kinase 1 Inhibitor II)
PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种有效,选择性,可逆和鞘氨醇竞争性 SPHK1 抑制剂,IC50 为 2 nM,Ki 为 3.6 nM。PF-543 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 还是有效的全血中 1-磷酸鞘氨醇 (S1P) 形成的有效抑制剂,IC50 为 26.7 nM。PF-543 诱导细胞凋亡,坏死和自噬。
PF-543 Chemical Structure
CAS No. : 1415562-82-1
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是否有货 |
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100 mg |
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250 mg |
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500 mg |
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* Please select Quantity before adding items.
PF-543 的其他形式现货产品:
PF-543 Citrate
生物活性 |
PF-543 (Sphingosine Kinase 1 Inhibitor II) 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 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy[1][2][3].
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IC50 & Target |
IC50: 2 nM (SPHK1); 26.7 nM (Sphingosine 1-phosphate (S1P))[1] Ki: 3.6 nM (SPHK1)[1]
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体外研究 (In Vitro) |
PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations[2]. PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity[2]. PF-543 inhibits C17-S1P formation in 1483 cells with an IC50 of 1.0 nM[1]. SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC50 concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[2]
Cell Line: |
Human pulmonary arterial smooth muscle (PASM) cells |
Concentration: |
10 nM, 100 nM, 1000 nM |
Incubation Time: |
24 hours |
Result: |
Abolished SK1 expression at nM concentrations. |
Apoptosis Analysis[2]
Cell Line: |
Human pulmonary arterial smooth muscle (PASM) cells |
Concentration: |
0.1 μM, 1 μM, 10 μM |
Incubation Time: |
24 hours |
Result: |
Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells. |
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体内研究 (In Vivo) |
PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2[2]. Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T1/2 is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension[2] |
Dosage: |
1 mg/kg |
Administration: |
Intraperitoneal injection; every second day; for 21 days |
Result: |
Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2. |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献 |
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[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]. 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.
[3]. Hamada M, et al. Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells. Cell Death Discov. 2017 Aug 14;3:17047.
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