ARUK2002821

ARUK2002821 : Inhibitor of PIP4K2A

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe ARUK2002821 is in the process of SERP review.

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Information

PIP4K2A

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P48426

Target Class: Kinase

Target SubClass: PIP family

Potency: IC50

Potency Value: 10 nM

Potency Assay: ADP-Glo assay

PDB ID for probe-target interaction (3D structure): 8C8C

Target aliases:

Phosphatidylinositol 5-phosphate 4-kinase type-2 a ...

DOI Reference: 10.1039/D3MD00039G

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): Selective against isoforms PI5P4Kγ(IC50 >39 uM) and PI5P4Kβ (IC50 ND). ARUK2002821 was profiled against 140 protein kinases and 15 lipid kinases. When tested at 1 μM in the lipid kinase screen the only target with <50% residual activity was PI5P4Kα (15.6%) and the considerable drop to the next most inhibited target indicated high specificity (SPHK2; 81.7% residual activity). In the protein kinase screen, no targets were inhibited by >50% at 1 μM; the lowest residual activities observed were for ERK1 and JAK3 (62 and 63%, respectively).

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

The compound has been profiled against a panel of around 155 kinases and demonstrated good selectivity. No screened kinase showed >50% inhibition at 1μm, except the target PIP5K2a(PI5P4Ka) showing 85% inhibition. The inhibitor is isoform selective. The co-crystal structure has been solved demonstrating the binding mode. The compound should be used together with probe BAY-091 as orthogonal tool compound.

(last updated: 17 Jun 2024 )