AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).

AZD8186 is an inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ.

Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM.

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity.

Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach.

NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor.

Umbralisib sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach.

PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM.

PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.

PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively.

PQR530 is a selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor.

SF2523 is a highly selective and potent inhibitor of PI3K and BRD4with IC50 values of 16 and 241 nM for PI3Kα and BD1, respectively.

TAK-117(INK1117,MLN1117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity.

FAPL-PI3Ki1 is a specific FAP-targeted PI3K inhibitor that selectively targets FAP-expressing human IPF lung fibroblasts and potently inhibits collagen synthesis.FAPL-PI3Ki1 significantly inhibited phosphorylation of Akt in IPF fibroblasts with IC50 of 200 nM, also inhibited phosphorylation of 4E-BP1.FAPL-PI3Ki1 induced suppression of TGFb1-stimulated collagen production and phosphorylation of Akt in IPF fibroblasts requires participation of FAP.FAPL-PI3Ki1 suppressed production of hydroxyproline (major building block of collagen), reduced collagen deposition, and increased mouse survival in a mouse model of IPF inhibited PI3K activation in fibrotic lungs.

CPL302-253 is a potent, selective inhibitor of PI3Kδ with IC50 of 12.2 nM and Kd of 0.83 nM, >350-fold selectivity over PI3K isoforms α, β, and γ (IC50>4,500 nM); CPL302-253 displays no off-target interaction in KinomeScan assays. CLP302-253 blocks activation of primary lymphoid cells in vitro, blocks IL-33 cytokine production in epithelial and T cell co-cultures. CLP302-253 bocks eosinophil infiltration to the lungs and IL-33 expression in HDM induced asthma mouse model.

Viridin is a secondary metabolite and naturally occurring furanosteroid. Viridin is potent inhibitor of the lipid kinase PI3K.

PI3Kδ/γ-IN-1 is a potent, selective PI3K-δ/γ inhibitor for treatment of hematological malignancies.

PI3K-IN-26 is a potent PI3K inhibitor with an IC50 of 36 nM for SU-DHL-6 cells (WO2016066142A1, compound 1).

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis.

PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC50 values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K.

PI3K-IN-27 is a potent inhibitor of PI3K. PI3K belongs to a large family of lipid signaling kinase that plays key role in cellular process including cell growth, differentiation, migration and apoptosis. PI3K-IN-27 has the potential for the research of hyper-proliferative diseases like cancer and inflammation, or immune and autoimmune diseases (extracted from patent WO2021233227A1, compound 1).

PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.

PI3Ka-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC50 of 0.7 nM and 3.3 nM, respectively. PI3Ka-IN-5 can be used for the research of colorectal cancer.

TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.

TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β .

ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.