PI3KC2β Inhibitor

PI-103 is a potent 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 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.

PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC₅₀s of 11, 18 and 13 nM, respectively.

PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC₅₀ of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC₅₀ of 16 nM and 39 nM, respectively.

AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC₅₀ of 0.69 nM.

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.

PIK-124 is a thiazolidinone-based PI3Kγ-biased PI3K inhibitor, with an IC₅₀ of 3 nM against PI3Kγ. PIK-124 exhibits cross-reactivity with PI3Kα (IC₅₀ = 23 nM), PI3Kδ (IC₅₀ = 340 nM), PI3KC2α (IC₅₀ = 140 nM) and PI3KC2β (IC₅₀ = 370 nM). PIK-124 is applicable to breast cancer-related research.

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.

MIPS-21335 is a PI3KC2α inhibitor with an IC₅₀ of 7 nM. MIPS-21335 also inhibits PI3KC2β, p110α, p110β and p110δ, with IC₅₀ values of 43, 140, 386 and 742 nM, respectively. MIPS-21335 has antithrombotic effect. MIPS-21335 can be used for the researches of cardiovascular disease and metabolic disease, such as thrombosis and hyperlipidemia.

Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC₅₀ of 14 nM.

AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC₅₀s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.

PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar K_d toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.

A66 is a highly specific and selective p110α inhibitor with an IC₅₀ of 32 nM.

CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC₅₀ of 6 nM, and exhibits 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). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC₅₀ of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells.