VPS34-IN-4

VPS34-IN-4 : Inhibitor of PIK3C3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Probe VPS34-IN-4 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

PIK3C3

Inhibitor

In Vitro Validations

Uniprot ID: Q8NEB9

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 15nM

Potency Assay: KinaseGLO assay

PDB ID for probe-target interaction (3D structure): 5ENN

Target aliases:

Phosphatidylinositol 3-kinase catalytic subunit ty ...

DOI Reference: 10.1021/acsmedchemlett.5b00335

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: MAP3K7

Potency end-point : Activity 150nM

Probe Selectivity in Vitro:

Selective over other lipid and protein kinases (>100-fold against >280 kinases evaluated, except TAK1 and PI3Kδ, 10-fold and 40-fold, respectively)".

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

While the dose used for the PK/PD experiments was 10 mg/kg, the dose for in vivo efficiency was 50 mg/kg.

(last updated: 24 Feb 2026 )