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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V5023 | NSC-781406 | 1676893-24-5 | NSC781406 is a novel and highly potent dual inhibitor of PI3K and mTOR with an IC50of 2 nM for PI3Kα. |
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V0108 | NU7441 (KU57788) | 503468-95-9 | NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive inhibitor of DNA-PK (DNA-dependent protein kinase) with IC50 of 14 nM, has anticancer activity. |
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V0121 | Omipalisib (GSK2126458, GSK458) | 1086062-66-9 | Omipalisib (also called GSK-2126458, GSK-458), apyridylsulfonamide analog, is a potent, highly selective and orally bioavailable small-molecule inhibitor of phosphatidylinositol 3-kinase (PI3K)p110α/β/δ/γ with potential anticancer activity. |
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V81077 | Penetratin-PI3Kγ(126-150) | Penetratin-PI3Kγ(126-150) is a PI3Kγ peptide inhibitor that plays important roles in respiratory diseases. | |
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V4430 | PF-04979064 | 1220699-06-8 | PF-04979064 is a novel, potent and selectivePI3K/mTORdual kinase inhibitor withKis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively. |
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V0151 | PF-4989216 | 1276553-09-3 | PF-4989216 is a novel, potent, orally bioactive and selective small molecule inhibitor of PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity. |
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V69236 | Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) | 245126-95-8 | Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) is a phospholipid component of cell membranes. |
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V0107 | PI-103 | 371935-74-9 | PI-103 is a novel and potent multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, and has anticancer activity. |
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V30716 | PI-103 Hydrochloride | 371935-79-4 | PI-103 Hydrochloride (PI 103; PI103),the hydrochloride salt of PI-103, is a multi-targetedPI3K and mTOR inhibitorwith potential antineoplastic activity. |
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V0149 | PI-3065 | 955977-50-1 | PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity. |
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V21950 | PI3K inhibitor 1 | 371934-59-7 | PI3K-IN-32 (compound 35) is a potent PI3K p110α inhibitor (antagonist) with pIC50 of 6.85. |
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V69224 | PI3K-IN-19 hydrochloride | 2132943-80-5 | PI3K-IN-19 HCl is a phosphatidylinositol-3-kinase (PI3K) inhibitor disclosed in patent WO2017153220, step 5. |
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V69191 | PI3K-IN-2 | 1403458-28-5 | PI3K-IN-2 (compound 10) is an orally bioactive PI3Kβ/δ inhibitor (IC50=7.1/8.6 nM), with better selectivity than PI3Kσ and PI3Kγ (IC50=13/190 nM). |
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V70246 | PI3K-IN-22 | 1202884-94-3 | PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. |
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V69239 | PI3K-IN-23 | 2755651-17-1 | PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue that promotes glucose uptake with EC50 of 7.00 μM. |
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V69235 | PI3K-IN-29 | 2768005-77-0 | PI3K-IN-29 is a potent PI3K inhibitor. |
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V69205 | PI3K-IN-36 | 1401436-93-8 | PI3K-IN-36 (compound A36) is a potent PI3K inhibitor. |
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V81132 | PI3K-IN-41 | PI3K-IN-41 (compound 2) is a photocage compound and a photocage PI3K inhibitor (antagonist) with anti-cancer properties (IC50=18.92 nM). | |
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V69238 | PI3K-IN-46 | 304645-61-2 | PI3K-IN-46 (Intermediate 4) is an intermediate in the synthesis/preparation of PI3K inhibitors (2-iminozolinone vinyl fused benzene analogues). |
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V81133 | PI3K-IN-47 | PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50= 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, and 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ. |
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