pi3kα/pi3kγ

Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.

SAR-260301, an orally available and selective inhibitor of PI3Kβ [IC50: 23 nM].

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).

hSMG-1 inhibitor 11e is an effective and selective inhibitor of hSMG-1 (IC50 <0.05 nM) and can be used in studies about cancer treatment.

PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.

BGT226 (NVP-BGT226) is a novel dual PI3K mTOR inhibitor, targeting PI3K α, β, and γ with IC50 values of 4 nM, 63 nM, and 38 nM, respectively.

WAY-600 is a potent, ATP-competitive, and selective inhibitor of mTOR with an IC50 of 9 nM; it blocks mTORC1 P-S6K(T389) and mTORC2 P-AKT(S473) but not P-AKT(T308), and is selective for mTOR over PI3Kα (>100-fold) and PI3Kγ (>500-fold).

PF-04979064 is a potent and selective PI3K and mTOR dual kinase inhibitor, with Ki values of 0.13 nM and 1.42 nM, respectively.

hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα γ (IC50=92 60 nM) and CDK1 CDK2 (IC50=32 7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.

CNX-1351 is a potent, isoform-selective, and targeted covalent inhibitor of PI3Kα.

Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.

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

Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)

PI3K Inhibitor ZSTK474 is an orally available, s-triazine derivative, ATP-competitive phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

AS-252424 is a potent and selective inhibitor of PI3Kγ with an IC50 of 33 nM and demonstrates over 10-fold selectivity for PI3Kγ versus PI3Kα.

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.

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

ON 146040 is an effective inhibitor of PI3K isoforms with IC50s of 14 and 20 nM for PI3Kα and PI3Kδ, respectively.

AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects.

NIBR-17 is a pan class I PI3K inhibitor. NIBR-17 inhibits PI3KKα, PI3KKβ, PI3KKγ, and PI3KKδ with IC50 of 1 nM, 9.2 nM, 9 nM, and 20 nM respectively.

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).

CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting over 10-1500 fold selectivity over other class I, II, and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM), and PI4KIIIB (IC50, 300.2 nM). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.

PARP PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.