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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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. |
|
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. |
|
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. | |
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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. |
|
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. |
|
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. |
|
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. |
|
V102103 | PI3K-IN-11 | 884539-95-1 | PI3K-IN-11 (Compound 13) is a PI3K inhibitor that selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50 of 6.4, 13, 8, and 11 nM, respectively), but does not inhibit mTOR (IC50=2.9 μM). |
|
V101842 | PI3K-IN-18 dihydrochloride | 1188890-32-5 | PI3K-IN-18 (Compound 1) dihydrochloride is a 4-morpholine-2-phenylquinazoline derivative and an inhibitor of PI3K p110α. |
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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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