PF-543 hydrochloride 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂,对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂,诱导细胞凋亡、坏死和自噬。
产品描述
PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
体外活性
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.
体内活性
PF543 was found to be a potent inhibitor (IC50 = 26.7 nM) capable of blocking >90% of C17-S1P formation in the blood.
Cas No.
1706522-79-3
分子式
C27H32ClNO4S
分子量
502.07
别名
PF-543
储存和溶解度
DMSO:90 mg/mL (136.83mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years