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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V0217 | MLS-2052 (GSK-3 Inhibitor IX; BIO) | 667463-62-9 | MLS2052 (also known as BIO, GSK3 Inhibitor IX, 6-Bromoindirubin-3-oxime) is a novel, potent,cell-permeable bis-indolo and specific inhibitor of GSK-3 (glycogen synthase kinase-3) with potential antitumor activity. |
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V121460 | (2S)-SB02024 | 2126737-29-7 | (2S)-SB02024 is a Vps34 inhibitor. |
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V121487 | (3aS,4R,9bR)-G-1 | 925419-53-0 | (3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. |
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V99779 | (R)-CCG-1423 | 2309931-09-5 | (R)-CCG-1423 is an inhibitor of RhoA. |
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V93367 | (Rac)-AZD8186 | 1296270-45-5 | (Rac)-AZD8186 is the racemate of AZD8186, a PI3K inhibitor that inhibits PI3Kβ (IC50=4 nM), PI3Kδ (IC50=12 nM), PI3Kα (IC50=35 nM), and PI3Kγ (IC50=675 nM). |
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V122208 | (S)-PI3K-IN-2 | 1403458-27-4 | (S)-PI3K-IN-2 is the enantiomer of PI3K-IN-2 and is a PI3Kβ/δ inhibitor with IC50 values of 0.198 and 0.282 μM, respectively. |
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V70263 | (S)-PI3Kα-IN-4 | 2322293-84-3 | (S)-PI3Kα-IN-4 is a potent PI3Kα inhibitor (antagonist) with IC50 of 2.3 nM. |
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V102881 | 17β-Hydroxywortmannin | 58053-83-1 | 17β-Hydroxywortmannin (Wortmannin-17β-ol) is an orally active PI-3-kinase inhibitor with IC50 of 0.5 nM. |
![2,4-Dichlorothieno[3,2-d]pyrimidine](http://www.invivochem.com/upload/1124/V124087.png)
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V124087 | 2,4-Dichlorothieno[3,2-d]pyrimidine | 16234-14-3 | 2,4-Dichlorothieno[3,2-d]pyrimidine is a thiophene-pyrimidine skeleton compound and an important synthetic precursor, widely used in the construction of 4-arylthiophene-[3,2-d]pyrimidine compounds. |
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V0129 | TG100-115 | 677297-51-7 | TG100-115 is a novel, potent and selective PI3Kγ/δ inhibitor with potential cardioprotecting effects. |
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V0142 | TG100713 | 925705-73-3 | TG100713 is a novel and potent pan-PI3K(phosphatidylinositol 3-kinase)inhibitor with potential anti-inflammatory activity. |
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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. |
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V126529 | 4-Vinylcyclohexene dioxide | 106-87-6 | 4-Vinylcyclohexene dioxide is an orally active metabolite of 4-vinylcyclohexene. |
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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. |
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V0118 | A66 | 1166227-08-2 | A66 is a novel, potent,reversible, ATP-competitive and highly selective p110α inhibitor with potential anticancer activity. |
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V69227 | Acetyl-Exenatide | 305815-28-5 | Acetyl-Exenatide is an acetylated analogue of Exenatide. |
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V114241 | AM-1430 | 1975263-74-1 | AM-1430 is a highly effective, selective, and orally available small molecule inhibitor of PI3Kδ with an IC50 value of 4.6 nM. |
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V69213 | Amdizalisib (HMPL-689) | 1894229-05-0 | Amdizalisib (HMPL-689) is a PI3K inhibitor used to study inflammation, autoimmune diseases, or cancer. |
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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. |
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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. |
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