PIKfyve-IN-1

• CAT Number: I042817
• CAS Number: 2857982-26-2
• Molecular Formula: C20H21N5
• Molecular Weight: 331.41
• Purity: ≥95%
• Synonyms: 16-[3-(dimethylamino)prop-1-ynyl]-3,5,12-triazatetracyclo[9.7.0.02,7.013,18]octadeca-1(11),2,4,6,13(18),14,16-heptaen-4-amine
• InChI: InChI=1S/C20H21N5/c1-25(2)10-4-5-13-8-9-16-15(11-13)18-17(23-16)7-3-6-14-12-22-20(21)24-19(14)18/h8-9,11-12,23H,3,6-7,10H2,1-2H3,(H2,21,22,24)
• InChIKey: DORZPJWJOBMQKC-UHFFFAOYSA-N
• SMILES: CN(C)CC#CC1=CC2=C(C=C1)NC3=C2C4=NC(=NC=C4CCC3)N

PIKfyve-IN-1 is a highly potent and cell-active chemical probe that inhibits phosphatidylinositol-3phosphate 5-kinase (PIKfyve) with IC50 value of 6.9 nM. PIKfyve-IN-1 can be used for the research of PIKfyve in virology[1]. PIKfyve-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PIKfyve-IN-1 inhibits PIKfyve in PIKfyve enzymatic assay and PIKfyve NanoBRET assay with IC50 values of 6.9 nM and 4.01 nM, respectively[1].
PIKfyve-IN-1 (0-10 μM) disrupts multiple phases of the lifecycle of coronaviruses: viral replication and viral entry[1].
PIKfyve-IN-1 inhibits MHV replication and SARS-CoV-2 replication with IC50 values of 23.5 nM and 19.5 nM, respectively[1].
PIKfyve-IN-1 (5 μM) impacts lysosomal homeostasis[1].

Reference

[1]. David H Drewry, et al. Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses. J Med Chem
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