| Identification | Back Directory | [Name]
1H-Indole-3-carboxaldehyde, 2-[4-(4-morpholinyl)-6-(phenylamino)-1,3,5-triazin-2-yl]hydrazone | [CAS]
232935-92-1 | [Synonyms]
1H-Indole-3-carboxaldehyde, 2-[4-(4-morpholinyl)-6-(phenylamino)-1,3,5-triazin-2-yl]hydrazone | [Molecular Formula]
C22H22N8O | [MOL File]
232935-92-1.mol | [Molecular Weight]
414.46 |
| Chemical Properties | Back Directory | [Boiling point ]
706.4±70.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
15.66±0.30(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
WX8 (Ro 91-4714) is an ATP-competitive PIKFYVE inhibitor, with Kd values of 0.9 nM and 340 nM for PIKFYVE and PIP4K2C, respectively. WX8 (Ro 91-4714) inhibits lysosomal fission without effecting homotypic lysosomal fusion. WX8 (Ro 91-4714) is used in the research of autophagy-dependent cancer[1]. | [Biological Activity]
WX8 (Ro 91-4714) is a selective phosphoinositide kinase PIKfyve inhibitor th at disrupts lysosome fission via tubulationlysosomal traffickingand heterotypic lysosomes-autophagosomes fusion (0.1-1 μM; U2OS)but not homotypic lysosome fusion. WX8 exhibits cancer-selective antiproliferation activity (IC50 = 48 nM/A375200 nM/U2OS; IC50 >10 μM/non-cancer 293T & HFF) with a higher potency than the PIKfyve inhibitor YM201636or the lysosomal inhibitors chloroquine & hydroxychloroquine (A375 IC50 = 119 nM1.7 μM1.9 μMrepectively). | [References]
[1] Ajit Roy, et al. Selective Termination of Autophagy-Dependent Cancers. Cells. 2024 Jun 25;13(13):1096. DOI:10.3390/cells13131096
[2] Gaurav Sharma, et al. A family of PIKFYVE inhibitors with therapeutic potential against autophagy-dependent cancer cells disrupt multiple events in lysosome homeostasis. Autophagy. 2019 Oct;15(10):1694-1718. DOI:10.1080/15548627.2019.1586257 |
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| Company Name: |
Merck KGaA
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21-20338288 |
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www.sigmaaldrich.cn |
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