pi3kδ

PI3Kδ-IN-15 is a selective PI3Kδ inhibitor that inhibits PI3Kδ more than 30-fold more effectively than PI3Kγ, PI3Kβ, and PI3Kα.

IHMT-PI3Kδ-372 is a selective inhibitor of PI3Kδ with an IC50 of 14 nM and can be used in studies about chronic obstructive pulmonary disease.

PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

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.

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

GSK2292767 is a potent and selective inhibitor of PI3Kδ.

GSK2292767 FA is a potent and selective inhibitor of PI3Kδ (pIC50 : 10.1).GSK2292767 FA is more than 500-fold more selective than other PI3K isoforms.GSK2292767 FA can be used in the study of respiratory diseases.

CZC24832 is a selective inhibitor of PI 3-kinase γ.

AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50 Ki: 87.8 nM).

PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.

Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.

Acalisib (CAL-120) (GS-9820) is a potent and selective inhibitor of PI3Kδ.

Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.

Umbralisib hydrochloride is a novel PI3Kδ inhibitor (IC50 and EC50 of 22.2 nM and 24.3 nM, respectively). Umbralisib hydrochloride is also active against CK1ε (EC50: 6.0 μM).

Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.

PI3Kδ-IN-23 (compound A11) is a potent inhibitor of PI3Kδ, with an IC50 of 0.27 nM. It binds to PI3Kδ through covalent interaction with Lys779 and plays a significant role in cancer research.

PI3Kδ BET-IN-1 (compound 10b) exhibits excellent and balanced activity against PI3Kδ (IC50= 112 nM) and BRD4-BD1 (IC50= 19 nM), while also demonstrating strong antiproliferative effects in DLBCL cells.

GNE-490 is an effective inhibitor of pan-PI3K with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50 = 750 nM).

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K mTOR. Activation of the PI3K mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.

PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .

IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).

TG100-115 is a PI3Kγ δ inhibitor (IC50: 83 235 nM), with fewer effects on PI3Kα β.