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 |
|---|---|---|---|---|
|
V69191 | PI3K-IN-2 | 1403458-28-5 | PI3K-IN-2 (compound 10) is an orally bioactive PI3Kβ/δ inhibitor (IC50=7.1/8.6 nM), with better selectivity than PI3Kσ and PI3Kγ (IC50=13/190 nM). |
|
V70246 | PI3K-IN-22 | 1202884-94-3 | PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. |
|
V69239 | PI3K-IN-23 | 2755651-17-1 | PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue that promotes glucose uptake with EC50 of 7.00 μM. |
|
V69235 | PI3K-IN-29 | 2768005-77-0 | PI3K-IN-29 is a potent PI3K inhibitor. |
|
V69205 | PI3K-IN-36 | 1401436-93-8 | PI3K-IN-36 (compound A36) is a potent PI3K inhibitor. |
|
V81132 | PI3K-IN-41 | PI3K-IN-41 (compound 2) is a photocage compound and a photocage PI3K inhibitor (antagonist) with anti-cancer properties (IC50=18.92 nM). | |
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V69238 | PI3K-IN-46 | 304645-61-2 | PI3K-IN-46 (Intermediate 4) is an intermediate in the synthesis/preparation of PI3K inhibitors (2-iminozolinone vinyl fused benzene analogues). |
|
V81133 | PI3K-IN-47 | PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50= 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, and 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ. | |
|
V85025 | PI3K-IN-49 | 2922415-69-6 | |
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V84865 | PI3K-IN-50 | 3023536-43-5 | |
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V84606 | PI3K-IN-51 | 2055765-77-8 | |
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V92110 | PI3K-IN-54 | 1336890-05-1 | PI3K-IN-54 (compound 10w) is a pan-PI3K inhibitor. |
|
V69189 | PI3K/HDAC-IN-1 | 2361418-52-0 | PI3K/HDAC-IN-1 is a potent (PI3K/HDAC) dual (bifunctional) inhibitor that efficiently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM respectively. |
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V85594 | PI3K/HDAC-IN-3 | 3006905-22-9 | |
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V69200 | PI3K/mTOR Inhibitor-11 | 2845104-25-6 | PI3K/mTOR Inhibitor-11 is an orally bioactive PI3K/mTOR inhibitor (IC50 for PI3Kα, PI3Kδ and mTOR are 3.5, 4.6 and 21.3 nM, respectively). |
|
V70243 | PI3K/mTOR Inhibitor-12 | 2891692-83-2 | PI3K/mTOR Inhibitor-12 is an orally bioavailable and selective PI3K/mTOR inhibitor (antagonist) with IC50s of 0.06 nM and 3.12 nM for PI3Kα and mTOR respectively. |
|
V69241 | PI3K/mTOR Inhibitor-13 | 1621718-37-3 | PI3K/mTOR Inhibitor-13 is an orally bioactive dual (bifunctional) inhibitor of phosphoinositide 3-kinase (PI3K) and mTOR kinase. |
|
V69207 | PI3K/mTOR Inhibitor-13 sodium | 2361009-23-4 | PI3K/mTOR Inhibitor-13 sodium is an orally bioactive dual (bifunctional) inhibitor of phosphoinositide 3-kinase (PI3K) and mTOR kinase. |
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V69214 | PI3K/mTOR Inhibitor-14 | 2919684-77-6 | PI3K/mTOR Inhibitor-14 (Compound Y-2) is a potent dual (bifunctional) inhibitor of PI3K and mTOR with IC50 of 171.4 nM and 10.1 nM respectively. |
|
V105205 | PI3K/mTOR Inhibitor-17 | PI3K/mTOR inhibitor-17 (compound 5nh) is a potent PI3K/mTOR inhibitor with inhibitory concentrations of 0.45 nM and 2.9 nM for PI3Kα and mTOR, respectively. |
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