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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V2910 | ETP-46321 | 1252594-99-2 | ETP-46321 is a novel, potent and orally bioavailable inhibitor of PI3Kα and PI3Kδ with Kiappvalues of 2.3 nM and 14.2 nM, respectively inbiochemical assays. |
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V69223 | ETP-47037 | 1316760-76-5 | ETP-47037 is a potent inhibitor of PI3Kα isoforms with IC50 of 0.99 nM. |
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V69233 | FAP-PI3KI1 | 2415941-98-7 | FAP-PI3KI1 is a fibroblast activation protein (FAP)-targeted PI3K inhibitor that can selectively target human idiopathic pulmonary fibrosis (IPF) cells expressing FAP and effectively inhibit collagen synthesis and reduce collagen deposition. |
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V69226 | FD2056 | 2685870-87-3 | FD2056 is a potent orally bioactive PI3K inhibitor. |
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V69197 | FD274 | 2641899-38-7 | FD274 is a potent dual (bifunctional) inhibitor of PI3K/mTOR, with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM and 2.03 nM for PI3Kα/β/γ/δ and mTOR respectively. |
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V69202 | Gallein (alizarin violet; Pyrogallol phthalein) | 2103-64-2 | Gallein is an inhibitor (blocker/antagonist) of G protein βγ (Gβγ) subunit signaling. |
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V4526 | GDC-0326 | 1282514-88-8 | GDC-0326 is a novel, potent and selectivePI3Kα (α-Isoform of Phosphoinositide 3-Kinase)inhibitor with aKiof 0.2 nM. |
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V70264 | Gilmelisib | 1845777-61-8 | This product is discontinued due to commercial reason. Gilmelisib is an antitumor active molecule. |
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V0146 | GNE-317 | 1394076-92-6 | GNE-317, an oxetane analog of GDC-0980, is a novel, potent, and selective PI3K/mTOR dual inhibitor with excellent BBB (blood-brain barrier) penetrating ability. |
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V4333 | GNE-477 | 1032754-81-6 | GNE-477 is a novel, potent and efficacious dual inhibitor ofPI3K(IC50=4 nM)/mTOR(Ki=21 nM). |
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V0126 | GSK1059615 | 958852-01-2 | GSK1059615 is a novel, potent and reversible inhibitor of P13K (phosphatidylinositol-3-kinases) with potential anticancer activity. |
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V2546 | GSK2292767 | 1254036-66-2 | GSK2292767 is a novel and selective PI3Kδ inhibitor being investigator for the treatment of respiratory diseases such as asthma and COPD. |
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V0135 | GSK2636771 | 1372540-25-4 | GSK2636771 is a novel, potent, selective and orally bioavailable inhibitor of PI3Kβ (phosphatidylinositol 3-kinase β)with potential anticancer activity. |
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V0148 | HS-173 | 1276110-06-5 | HS-173 is a novel and potent PI3Kα (phosphatidylinositol 3-kinase) inhibitor (IC50 = 0.8 nM) with a potential to be used asan effective therapeutic agent for ameliorating liver fibrosis. |
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V103314 | Hydroxy celecoxib | 170571-00-3 | Hydroxycelecoxib, a derivative of celecoxib, is a PI3K/Akt signaling pathway activator that promotes epithelial repair. |
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V0110 | IC-87114 | 371242-69-2 | IC-87114 is a novel, potent, selective andATP-competitive PI3Kδ inhibitor (p110delta-selective) with potential anticancer activity. |
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V97283 | IHMT-PI3K-315 | IHMT-PI3K-315 (20e) is a potent and selective PI3Kγ/δ inhibitor with IC50 values of 4.0 and 9.1 nM for PI3Kγ and PI3Kδ, respectively. | |
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V80354 | IHMT-PI3K-455 | IHMT-PI3K-455 (Compound 15u) is a specific and orally bioactive dual PI3Kγ/δ inhibitor. | |
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V76896 | iMDK quarterhydrate | iMDK quarterhydrate is a potent PI3K inhibitor that suppresses the growth factor MDK (also known as midkine or MK). | |
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V3109 | IPI-3063 | 1425043-73-7 | IPI-3063 is a potent and selective PI3Kp110δinhibitor with IC50 of 2.5 ± 1.2 nM and IC50 values of >1000 nM for other classes of PI3K isoforms (p110α, p110β, p110γ). |