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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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. |
|
V69198 | PI3K/mTOR Inhibitor-4 | 2361215-32-7 | PI3K/mTOR Inhibitor-4 is a pan-class I PI3K/mTOR inhibitor (antagonist) with orally bioactive. |
|
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 | 2966861-50-5 | 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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V85853 | PI3Kα-IN-15 | 2893920-80-2 | |
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V84488 | PI3Kα-IN-16 | 1448711-61-2 | |
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V84016 | PI3Kα-IN-17 | 2935973-28-5 | |
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V92042 | PI3Kα-IN-19 | 885692-56-8 | PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor that targets the binding site at the p110α catalytic subunit. |
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V103793 | PI3Kα-IN-22 | 2925030-26-6 | PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective PI3KαH1047R inhibitor with IC50 of 1 nM in pAKT T47D AlphaLISA. |
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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. |
|
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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V81138 | PI3Kδ-IN-14 | PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50= 0.8 nM, K d: 84.8 nM). |
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