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You are here:Home-Inhibitors & Agonists-PI3K/Akt/mTOR Pathway-PI3K

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PI3K (Phosphoinositide 3-kinase), via phosphorylation of the inositol lipid phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), forms the second messenger molecule phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P3) which recruits and activates pleckstrin homology domain containing proteins, leading to downstream signalling events crucial for proliferation, survival and migration. Class I PI3K enzymes consist of four distinct catalytic isoforms, PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ.

There are three major classes of PI3K enzymes, being class IA widely associated to cancer. Class IA PI3K are heterodimeric lipid kinases composed of a catalytic subunit (p110α, p110β, or p110δ; encoded by PIK3CA, PIK3CB, and PIK3CD genes, respectively) and a regulatory subunit (p85).

The PI3K pathway plays an important role in many biological processes, including cell cycle progression, cell growth, survival, actin rearrangement and migration, and intracellular vesicular transport.

Cat. No. Product Name CAS No. Information
H9570

Izorlisib

 		1007207-67-1

Izorlisib(CH5132799) is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
H9563

Gilmelisib

 		1845777-61-8

Gilmelisib is an antineoplastic. Gilmelisib is a PI3K inhibitor( IC50 of <1 nM for PI3K p110α).
H9449

Amdizalisib

 		1894229-05-0

Amdizalisib is a potent phosphatidylinositol 3-kinase (PI3K) inhibitor.
H9035

MCX83

 		1414453-79-4

MCX 83 is a highly potent, selective and orally bioavailable PI3K/mTOR inhibitor with IC50 values of 0.8 nM/3.3 nM;MCX 83 presented remarkable selectivity against a panel of 468 kinases,high in vitro metabolic stability, and favorable pharmacokinetic parameters without significant CYP450 and h-ERG binding inhibition.
H9033

PI3K inhibitor 32

 		1258017-82-1

PI3K inhibitor 32 is a highly potent, subtype selective, and CNS penetrant PI3Kγ inhibitor with Ki of 3 nM,showed good MDCK-MDR1 cell permeability;PI3K inhibitor 32 had the best brain-to-plasma ratio in rats (B/P) as a result of the low MDCK-MDR1 efflux ratio (0.9) and high permeability. The higher lipophilicity (cLogD 3.2) attributed compound 32 accounts for good permeability.
H9032

PI3K inhibitor 14

 		1258017-30-9

PI3K inhibitor 14 is a novel,an oral series of potent and selective alkynylthiazole-derived PI3Kγ inhibitor with Ki of 3 nM,showed good MDCK-MDR1 cell permeability;Compound 14 showed robust inhibition of PI3Kγ mediated neutrophil migration in vivo.
H8980

Zandelisib

 		1401436-95-0

Zandelisib (ME-401) is an oral, once-daily, selective inhibitor of phosphatidylinositol 3-kinase delta (PI3Kδ) in clinical development for the treatment of B-cell malignancies.
H8747

Linperlisib

 		1702816-75-8

Linperlisib is a potent and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, has an IC50 of 6.4 nM.
H7097

ZSTK-474

 		475110-96-4

A potent inhibitor of class I PI3K isoforms with IC50 of 17 nM, 53 nM, and 6 nM for p110β, p110γ, and p110δ, respectively; shows potent antiproliferative activity against a panel of 39 human cancer cell lines with mean GI50 of 0.32 uM, more effectively than that of LY294002 or wortmannin; induces apoptosis in OVCAR3 cells, and induces complete G1-phase arrest but not apoptosis in A549 cells at 10 uM; completely inhibits the growth of A549, PC-3, and WiDr xenografts in mice at 400mg/kg; and induces the regression of A549 xenograft tumors.
H7095

Wortmannin

 		19545-26-7

A potent PI3K inhibitor with IC50 3 nM, does not inhibit PI4K activity; inhibits both Fc epsilon RI-mediated histamine secretion and leukotriene release up to 80% with IC50 of 2.0 and 3.0 nM, respectively; Also inhibits DNA-PK and MLCK.

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