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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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). |
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V87885 | KTC1101 | 2764833-47-6 | KTC1101 is an orally active pan-PI3K inhibitor. |
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V0103 | LY294002 | 154447-36-6 | LY294002,a morpholine-containing compound designed based on the flavonoid quercetin,is apotent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively. |
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V69220 | MCX 28 | 1414453-58-9 | MCX 28 is a PI3K/mTOR/PIM inhibitor showing low nanomolar activity. |
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V25217 | ME-401 (P110δ-IN-1 ) | 1595129-71-7 | PWT143, formerly known as ME-401, is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity. |
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V115557 | ML-220 | 662151-10-2 | ML-220 is a PI3K modulator that can be used in research on tumors and infectious diseases. |
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V2898 | MLN-1117 | 1268454-23-4 | Serabelisib (formerly known as INK-1117, MLN-1117, and/or TAK-117) is a potent, selective, and oral bioavailable inhibitor of PI3Kα (phosphoinositide 3-kinase) isoform with IC50 of 21 nmol/L against PI3Kα. |
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V94330 | Nemiralisib succinate | 1364799-98-3 | Nemiralisib Succinate is a potent and selective PI3Kδ inhibitor with a pKi of 9.9. |
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V98364 | Nic-15 | 2896739-91-4 | Nic-15 (compound 4n) is an anticontractile agent used to antagonize the hypovascular properties of pancreatic tumors. |
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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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V103791 | OMS14 | OMS14 has inhibitory effects on phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, inhibiting 19% PI3Kγ and 65% PIK3CD/PIK3R1 activities at 100 μM. |