IOA-244

IOA-244 : non-ATP competitive inhibitor of PIK3CD

Structure

SERP Rating

Probe IOA-244 is in the process of SERP review.

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Information

PIK3CD

non-ATP competitive

up to 1 uM

In Vitro Validations

Uniprot ID: O00329

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 142 nM

Potency Assay: Scintillation Proximity Assay (SPA)

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

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1158/2767-9764.CRC-22-0477

Uniprot ID: O00329

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: Ki

Potency Value: 82 nM

Potency Assay: ATP competition assay

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

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1158/2767-9764.CRC-22-0477

Uniprot ID: O00329

Target Class: Kinase

Target SubClass: PI3/PI4

Potency: IC50

Potency Value: 19 nM

Potency Assay: Kinativ on Jurkat cell lisate

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

Target aliases:

Phosphatidylinositol 4,5-bisphosphate 3-kinase cat ...

DOI Reference: 10.1158/2767-9764.CRC-22-0477

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity in Jurkat cell lysate was measured using the KiNativ method at 10 uM.

Probe Selectivity in Vitro:

Selective against Isoforms: IC50 PI3Kα 10.1 μM, IC50 PI3Kβ 0.43 μM, IC50 PI3Kγ >15 μM

Potency assay (off target): The same KiNativ platform was also used to measure the potency and selectivity of IOA-244 in human whole blood lysate. IOA-244 was highly selective for PI3Kδ with an IC50 of 0.28 μmol/L. No other kinases were inhibited with an IC50 <30 μmol/L.

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SERP ratings and comments

No SERP comments found for IOA-244