PI3Kα Inhibitor

Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC₅₀s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC₅₀s=39, 113, 9 and 43?nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC₅₀=150?nM) and mTOR (IC₅₀=157?nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC₅₀s of 160 and 910 nM, respectively.

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.

Serabelisib (MLN1117) is a selective p110α inhibitor with an IC₅₀ of 15 nM.

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.

Flupentixol is an orally active D₁/D₂ dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC₅₀=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.

PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC₅₀s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively.

PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.

PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 hydrochloride induces apoptosis.

BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.

PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 induces apoptosis.

PI4K-IN-1 (compound 44) is a potent PI4KIII inhibitor, with pIC₅₀ values of 9.0 and 6.6 for PI4KIIIα and PI4KIIIβ, respectively. PI4K-IN-1 also inhibits PI3Kα/β/γ/δ, with pIC₅₀ values of 4.0/<3.7/5.0/<4.1, respectively.

Buparlisib Hydrochloride (BKM120 Hydrochloride) is a CNS-penetrant pan-class I PI3K inhibitor, with IC₅₀ of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.

Roginolisib (MSC2360844; IOA-244) is a potent, orally active and selective PI3Kδ inhibitor, with an IC₅₀ of 145 nM. Roginolisib shows highly selective against a panel of 278 additional kinases.

Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

BGT226 (NVP-BGT226 maleate) is a PI3K (with IC₅₀s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

Nemiralisib (GSK2269557 free base) is a potent and highly selective PI3Kδ inhibitor with a pK_i of 9.9.

AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC₅₀ of 18 nM.

SF2523 is a highly selective and potent inhibitor of PI3K with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.