selective pi3kδ inhibitor 1

Selective PI3Kδ Inhibitor 1 is a PI3Kδ Inhibitor( IC50 = 0.9 nM).

GS-9901 is a selective, orally active and potent PI3Kδ inhibitor (IC50: 1 nM) for the study of non-Hodgkin's lymphoma and chronic lymphocytic leukemia.

ATM Inhibitor-1 is a highly potent, selective, and orally active ATM inhibitor (IC50: 0.7 nM) with anti-tumor activity. It exhibits weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM), and PI3Kδ (IC50, 0.73 μM).

Parsaclisib (INCB050465) is a potent and selective inhibitor of PI3Kδ(IC50 of 1 nM at 1 mM ATP)

PI3Kdelta inhibitor 1 is a potent, selective and orally available inhibitor of PI3Kδ with an IC50 of 1.3 nM.

PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).

(S)-PI3Kα-IN-4, a potent inhibitor of PI3Kα with an IC50 of 2.3 nM, demonstrates 38.3-, 4.25-, and 4.93-fold selectivity over PI3Kβ, PI3Kδ, and PI3Kγ, respectively, and is suitable for cancer research[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1].

FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].

PI3Kδ γ-IN-1 is a selective and efficacious inhibitor of PI3Kδ γ, suitable for treating hematologic malignancies.

Umbralisib (TGR-1202) sulfate, an orally active compound, serves as a potent, selective inhibitor targeting both PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. It demonstrates unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL) and is applicable in the research of hematological malignancies.

IHMT-PI3K-455 (Compound 15u) is a potent, selective PI3Kγ δ dual inhibitor with IC50 values of 7.1 nM for PI3Kγ and 0.57 nM for PI3Kδ, exhibiting oral activity. This compound inhibits AKT phosphorylation and promotes tumor regression by recruiting and activating CD8+ T cells. It is utilized in cancer research [1].

PI3Kδ-IN-14 (Compound (S)-29), a selective PI3Kδ inhibitor with an IC50 of 0.8 nM and a Kd of 84.8 nM, targets the ATP-binding site within the kinase domain of PI3Kδ, exhibiting anti-inflammatory properties by impeding the PI3K AKT pathway and alleviating acute lung injury (ALI) [1].

Se15, a selective PI3Kδ inhibitor, exhibits potency with an IC50 value of less than 0.1nM and is utilized in autoimmune research [1].