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PF-543 hydrochloride (Synonyms: Sphingosine Kinase 1 Inhibitor II hydrochloride)
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 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 hydrochloride 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 hydrochloride 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 hydrochloride 诱导细胞凋亡,坏死和自噬。
PF-543 hydrochloride Chemical Structure
CAS No. : 1706522-79-3
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PF-543 hydrochloride 的其他形式现货产品:
生物活性 |
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) 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 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy[1][2][3]. |
IC50 & Target |
IC50: 2 nM (SPHK1); 26.7 nM (Sphingosine 1-phosphate (S1P))[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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis[2]
Apoptosis Analysis[2]
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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]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
502.07 |
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Formula |
C27H32ClNO4S |
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CAS 号 |
1706522-79-3 |
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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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