APY0201

APY0201 : Inhibitor of PIKFYVE

Structure

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Probe APY0201 is in the process of SERP review.

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Information

PIKFYVE

Inhibitor

up to 300 nM

Probe Availability:

In Vitro Validations

Uniprot ID: Q9Y2I7

Target Class: Kinase

Target SubClass: Serine Kinase

Potency: IC50

Potency Value: 5.4 nM

Potency Assay: Cell-free functional assay of full-length PIKfyve kinase

PDB ID for probe-target interaction (3D structure): --

Target aliases:

1-phosphatidylinositol 3-phosphate 5-kinase, PIP5K ...

DOI Reference: 10.1016/j.bmc.2014.03.036

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

In situ native kinase profiling approach (KiNativ profile) using an ATP-competitive probe and Jurkat cells lysate was used to determine the selectivity for 24 lipid kinases and 83 protein kinases at 300 nM. Other than PIKfyve, only the kinases ITPK1 and LOK consistently displayed >50% inhibition when treated with 300 nM of APY0201. APY0201 was submitted to Cerep (Seattle, WA) for evaluation by a receptor binding assay at 10 μM, with a panel of 137 G protein-coupled receptors (GPCRs), enzymes, ion channels, and transporters, and it showed negligible inhibitions relative to the IC50 value in the PIKfyve kinase assay.

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