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 |
|---|---|---|---|---|
|
V70263 | (S)-PI3Kα-IN-4 | 2322293-84-3 | (S)-PI3Kα-IN-4 is a potent PI3Kα inhibitor (antagonist) with IC50 of 2.3 nM. |
|
V0117 | 3-Methyladenine (3-MA; Autophagy Inhibitor) | 5142-23-4 | 3-Methyladenine (also called 3-MA; Autophagy Inhibitor) is a novel, potent,cell-permeable and selective PI3K inhibitor. |
|
V2540 | 740 Y-P (PDGFR 740Y-P) | 1236188-16-1 | 740 Y-P is a cell-permeable peptide acting as a phosphopeptide activator of PI3K. |
|
V0118 | A66 | 1166227-08-2 | A66 is a novel, potent,reversible, ATP-competitive and highly selective p110α inhibitor with potential anticancer activity. |
|
V4057 | Acalisib (GS-9820) | 870281-34-8 | Acalisib (formerly known asCAL-120;GS-9820) isa novel, potent and highly selective inhibitor ofp110δ[the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K)] with anticancer activities. |
|
V69227 | Acetyl-Exenatide | 305815-28-5 | Acetyl-Exenatide is an acetylated analogue of Exenatide. |
|
V0114 | Alpelisib (BLY-719; Piqray; NVP-BYL719) | 1217486-61-7 | Alpelisib (formerly also known as BLY719; trade name: Piqray) is a novel, potent, newly approved, orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with antineoplastic activity. |
|
V69213 | Amdizalisib (HMPL-689) | 1894229-05-0 | Amdizalisib (HMPL-689) is a PI3K inhibitor used to study inflammation, autoimmune diseases, or cancer. |
|
V11021 | AMG-511 | 1253573-53-3 | AMG-511 is a potent and selective pan class I PI3K inhibitor exhibiting IC50 of 8, 11, 2, and 6 nM against the PI3K β, α, β, and ≤ isoforms respectively. |
|
V0153 | AMG319 (ACP-319) | 1608125-21-8 | AMG319 (also known as ACP319) is a novel, potent, selective, orally bioavailable small molecule inhibitor of PI3Kδ (phosphoinositide-3 kinase δ)with potential anticancer activity. |
|
V78789 | Anticancer agent 137 | Anticancer agent 137 (8q) is a potent PI3k inhibitor. | |
|
V0125 | Apitolisib (GDC-0980, RG-7422, GNE-390) | 1032754-93-0 | Apitolisib (formerly also known as GDC0980, RG7422, GNE390) is a novel, potent, selective and orally bioavailable class I PI3K inhibitor with potential anticancer activity. |
|
V69231 | Apoptin-derived peptide | 2232156-31-7 | Apoptin-derived peptide is an anticancer active polypeptide with cytotoxic effect. |
|
V2333 | AS-041164 | 1146702-72-8 | AS-041164 is a potent, selective, orally bioactive PI3Kγ isoform inhibitor (antagonist) with IC50 of 70 nM. |
|
V0130 | AS-252424 | 900515-16-4 | AS-252424 is a novel, potent, orally bioactive and selective PI3Kγ inhibitor with potential anticancer activity. |
|
V0134 | AS-604850 | 648449-76-7 | AS-604850 is a novel, potent, selective, and ATP-competitive inhibitor of PI3Kγ (phosphatidylinositol 3-kinase γ) with IC50 of 250 nM and aKi of 180 nM. |
|
V0115 | AS-605240 | 648450-29-7 | AS-605240 is a novel, potent, orally bioactive andATP-competitiveinhibitor of PI3-kinase γ (PI3Kγ) with potential anti-inflammatory activity. |
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V2337 | AS041164 | 6318-41-8 | AS041164 is a novel and potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM) |
|
V69215 | ATM Inhibitor-3 | 2769140-52-3 | ATM Inhibitor -3 (Compound 34) is a potent and specific ATM inhibitor (antagonist) with IC50 of 0.71 nM. |
|
V69210 | ATM Inhibitor-4 | 2769140-74-9 | ATM Inhibitor -4 (Compound 39) is a potent and specific ATM inhibitor (antagonist) with IC50 of 0.32 nM. |
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