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PI-3065

Inhibitor of PIK3CD

Structure

Information

  • PIK3CD
  • Inhibitor
  • up to 500 nM

In Vitro Validations

Uniprot ID: O00329
Target Class: Lipid kinase
Target SubClass: Class I
Potency: Ki, IC50
Potency Value: 1.5 nM; 15 nM
Potency Assay: Enzymatic Activity
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: no
Target aliases:
Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selective against PI3K family members: p110alpha, beta and gamma (1.1, 2.3, 27.5 uM). No significant activity against 72 protein kinases was observed at ≤ 10 μM in a KinaseProfiler assay (Millipore).

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SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

PI-3065 is an older and well-studied PI3Kdelta inhibitor.  The compound lacks a negative control and overall, off-target evaluation is somewhat modest.  While the selectivity within the family has been established, the broader selectivity profile has not been fully elucidated.  As a tool in conjunction with several more recently published PI3Kdelta inhibitors of similar and more different structures, this compound can be used as one of several tools to interrogate PI3kdelta inhibition. In vivo, the levels of target engagement in relevant tissues and cell types have not been studied in detail and 75 mpk appears to modulate the target, there is insufficient dose-response and time-course data available to determine whether 75 mpk is indeed the best dose for this compound in mice. 

(last updated: 5 Jun 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 25 Jun 2021 )