Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one | i.e. CAL-101, highly selective and small molecule inhibitor of isoform PI3Kdelta. Inhibitor blocks constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O00329 | catalytic subunit delta isoform | - |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000025 | - |
isoform PI3Kdelta, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one | |
0.000089 | - |
isoform PI3Kgamma, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one | |
0.000565 | - |
isoform PI3Kbeta, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one | |
0.00082 | - |
isoform PI3Kalpha, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one |
General Information | Comment | Organism |
---|---|---|
physiological function | in tumor cell lines and primary patient samples representing multiple B-cell malignancies, constitutive phosphatidylinositol-3-kinase pathway activation is dependent on isoform PI3Kdelta. Inhibitor 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one blocks constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis | Homo sapiens |