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. The four distinct catalytic isoforms of class I PI3K enzymes are PI3K, PI3K, PI3K, and PI3K.
Three main classes of PI3K enzymes exist, with class IA being strongly linked to cancer. Catalytic subunits (p110α, p110β, or p110δ; encoded by PIK3CA, PIK3CB, and PIK3CD genes, respectively) and regulatory subunits (p85) make up heterodimeric lipid kinases known as class IA PI3K.
The PI3K pathway is crucial for the progression of the cell cycle, cell growth and survival, actin rearrangement and migration, and intracellular vesicular transport, among many other biological processes.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69189 | PI3K/HDAC-IN-1 | 2361418-52-0 | PI3K/HDAC-IN-1 is a potent (PI3K/HDAC) dual (bifunctional) inhibitor that efficiently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM respectively. |
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V69200 | PI3K/mTOR Inhibitor-11 | 2845104-25-6 | PI3K/mTOR Inhibitor-11 is an orally bioactive PI3K/mTOR inhibitor (IC50 for PI3Kα, PI3Kδ and mTOR are 3.5, 4.6 and 21.3 nM, respectively). |
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V70243 | PI3K/mTOR Inhibitor-12 | 2891692-83-2 | PI3K/mTOR Inhibitor-12 is an orally bioavailable and selective PI3K/mTOR inhibitor (antagonist) with IC50s of 0.06 nM and 3.12 nM for PI3Kα and mTOR respectively. |
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V69241 | PI3K/mTOR Inhibitor-13 | 1621718-37-3 | PI3K/mTOR Inhibitor-13 is an orally bioactive dual (bifunctional) inhibitor of phosphoinositide 3-kinase (PI3K) and mTOR kinase. |
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V69207 | PI3K/mTOR Inhibitor-13 sodium | 2361009-23-4 | PI3K/mTOR Inhibitor-13 sodium is an orally bioactive dual (bifunctional) inhibitor of phosphoinositide 3-kinase (PI3K) and mTOR kinase. |
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V69214 | PI3K/mTOR Inhibitor-14 | 2919684-77-6 | PI3K/mTOR Inhibitor-14 (Compound Y-2) is a potent dual (bifunctional) inhibitor of PI3K and mTOR with IC50 of 171.4 nM and 10.1 nM respectively. |
|
V4988 | PI3K/mTOR Inhibitor-2 | 1848242-58-9 | PI3K/mTOR Inhibitor-2 is a novel and potent dual pan-PI3K/mTORinhibitor with antitumor activity and withIC50values of 3.4/34/16/1 nM forPI3Kα/PI3Kβ/PI3Kδ/PI3Kγand 4.7 nM formTOR. |
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V69211 | PI3K/mTOR Inhibitor-3 | 1363338-53-7 | PI3K/mTOR Inhibitor-3 (compound 12) is an imidazoquinoline compound that is a potent dual (bifunctional) inhibitor of PI3K and mTOR. |
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V69198 | PI3K/mTOR Inhibitor-4 | 2361215-32-7 | PI3K/mTOR Inhibitor-4 is a pan-class I PI3K/mTOR inhibitor (antagonist) with orally bioactive. |
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V70265 | PI3Kα-IN-11 | 300803-79-6 | PI3Kα-IN-11 is a potent PI3Kα inhibitor (antagonist) with anti-cancer effect. |
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V81135 | PI3Kα-IN-12 | PI3Kα-IN-12 (compound 13) is a selective PI3Kα inhibitor (IC50= 1.2 nM). | |
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V70266 | PI3Kα-IN-13 | 2955529-67-4 | PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC50= 2.5 nM). |
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V81136 | PI3Kα-IN-14 | PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor (antagonist) with IC50 of 0.14 nM. | |
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V70262 | PI3Kα-IN-4 | 2322293-83-2 | PI3Kα-IN-4 is a specific and orally bioactive PI3Kα inhibitor (antagonist) with IC50 of 1.8 nM. |
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V69192 | PI3Kγ inhibitor 4 | 1821038-80-5 | PI3Kγ inhibitor 4 is a specific and orally bioactive PI3Kγ inhibitor (antagonist) with IC50 of 40 nM. |
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V69234 | PI3Kγ inhibitor 5 | 2566569-31-9 | PI3Kγ inhibitor 5 is an inhibitor (blocker/antagonist) of phosphoinositide 3-kinase gamma (PI3Kγ) with IC50 of 34 nM. |
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V69222 | PI3Kγ inhibitor 6 | 900515-01-7 | PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor. |
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V69196 | PI3Kγ inhibitor 7 | 2575863-25-9 | PI3Kγ inhibitor 7 (compound 2) is a potent orally bioactive PI3Kγ inhibitor (antagonist) with IC50s of 4768, 878.1, 3.42, and 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. |
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V81137 | PI3Kδ-IN-12 | PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC50 = 5.8), with pKis of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively. | |
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V69232 | PI3Kδ-IN-13 | 1686137-02-9 | PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM). |
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