货号:A451925 同义名: Sphingosine Kinase 1 Inhibitor II hydrochloride;PF-543 (hydrochloride)
PF-543 HCl is a cell-permeant inhibitor of SphK1 with a Ki of 3.6 nM, PF-543 is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
97% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
97% | |||||||||||||||||
Lys05 | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Sphingosine 1-phosphate (S1P) is an extracellular ligand that regulates endothelial cell function and angiogenesis, promotes survival and migration of cancer cells, and acts as a key regulator of immune cell trafficking. S1P is formed primarily by the action of sphingosine kinases (SphKs). PF 543 is a potent, cell-permeant inhibitor of SphK1 with an IC50 value of 2.0 ± 0.6nM in an in vitro enzyme assay and is able to inhibit the enzyme >95% at 20 nM. PF-543 was also able to inhibit C17-S1P formation in 1483 cells with an IC50 value of 1.0 ± 0.3nM. PF-543 showed 132-fold selectivity for SphK1 over SphK2 (IC50 = 356nM). The inhibition of SphK1 by PF-543 led to a concentration-dependent depletion of the intracellular level of S1P with an EC50 value of 8.4nM. The presence of 1μM PF-543 for 7 days in the culture medium resulted in a 10-fold decrease in S1P and a 2-fold increase in sphingosine levels in 1483 cells. PF543 also potently inhibited C17-S1P formation in human whole blood with an IC50 value of 26.7 nM[1]. PF-543 treatment (0.93mg/kg body weight per day) for 28 days significantly decreased erythrocyte Sphk1 activity and reduced erythrocyte and plasma S1P levels in SCD Tg mice[2]. |
作用机制 | PF 543 structurally resembles sphingosine and potentially could act as SphK1 substrate. It inhibits S1P binding to human recombinant SphK1 with a Ki value of 3.6nM[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.96mL 1.99mL 1.00mL |
19.92mL 3.98mL 1.99mL |
CAS号 | 1706522-79-3 |
分子式 | C27H32ClNO4S |
分子量 | 502.065 |
别名 | Sphingosine Kinase 1 Inhibitor II hydrochloride;PF-543 (hydrochloride);PF-543 hydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 | |
动物实验配方 |