产品名称
WX8, ≥98% (HPLC)
InChI key
NJIKLALXAPYTCW-BUVRLJJBSA-N
SMILES string
C1(NC2=CC=CC=C2)=NC(N/N=C/C3=CNC4=C3C=CC=C4)=NC(N5CCOCC5)=N1
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Selective phosphoinositide kinase PIKfyve inhibitor with higher antiproliferation potency in A375 cultures than YM201636, chloroquine or hydroxychloroquine.
WX8 (Ro 91-4714) is a selective phosphoinositide kinase PIKfyve inhibitor that disrupts lysosome fission via tubulation, lysosomal trafficking, and heterotypic lysosomes-autophagosomes fusion (0.1-1 µM; U2OS), but not homotypic lysosome fusion. WX8 exhibits cancer-selective antiproliferation activity (IC50 = 48 nM/A375, 200 nM/U2OS; IC50 >10 µM/non-cancer 293T & HFF) with a higher potency than the PIKfyve inhibitor YM201636, or the lysosomal inhibitors chloroquine & hydroxychloroquine (A375 IC50 = 119 nM, 1.7 µM, 1.9 µM, repectively).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Ajit Roy et al.
Molecular oncology, 18(4), 988-1011 (2024-02-28)
Inhibitors specifically targeting the 1-phosphatidylinositol 3-phosphate 5-kinase (PIKFYVE) disrupt lysosome homeostasis, thereby selectively terminating autophagy-dependent human cancer cells in vivo as well as in vitro without harming the viability of nonmalignant cells. To elucidate the mechanism by which PIKFYVE inhibition
Ajit Roy et al.
Autophagy, 19(9), 2464-2484 (2023-02-22)
Although PIKFYVE phosphoinositide kinase inhibitors can selectively eliminate PIKFYVE-dependent human cancer cells in vitro and in vivo, the basis for this selectivity has remained elusive. Here we show that the sensitivity of cells to the PIKFYVE inhibitor WX8 is not
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