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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V69203 | UCL-TRO-1938 | 2919575-27-0 | UCL-TRO-1938 is a potent allosteric activator of PI3Kα with EC50 of approximately 60 μM. |
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V0985 | VPS34 inhibitor 1 | 1383716-46-8 | VPS34 inhibitor 1 (also known as Vps34-IN1, Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 the potential to serve as a chemical tool to modulate autophagy in Vivo. |
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V69209 | Vps34-IN-3 | 2770104-92-0 | Vps34-IN-3 is an orally bioactive and selective VPS34 kinase inhibitor. |
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V4832 | VPS34-IN2 | 1383716-40-2 | VPS34-IN2 (PIK-III; Vps34-PIK-III) is a novel, potent and selective inhibitor ofVPS34 (IC50 = 18 nM) with the ability to modulate autophagy in Vivo. |
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V28052 | VPS34-IN1 | 1383716-33-3 | VPS34-IN1 (VPS34-IN-1) is a novel and potent Vps34 (vacuolar protein sorting 34) inhibitor with potential antitumor activity. |
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V0143 | VS-5584 (SB-2343) | 1246560-33-7 | VS-5584 (also known as SB2343), a purine analog, is a novel, potent and selective small-molecule dual inhibitor of both mammalian target of rapamycin (mTOR) kinase and all class I phosphoinostide 3-kinase (PI3K) isoforms with potential anticancer activity. |
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V115552 | X-370 | 1280725-80-5 | X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). |
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V0137 | YM201636 | 371942-69-7 | YM201636, apyridofuropyrimidine compound, is a novel, potent and selective PIKfyve (phosphatidylinositol‑3‑phosphate 5‑kinase) inhibitor with potential anti-retroviral replication and anticancer activity, as silencing of PIKfyve which is the sole enzyme for PtdIns(3,5)P(2) biosynthesis that controls proper endosome dynamics, can inhibit retroviral replication. |
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V0113 | ZSTK474 | 475110-96-4 | ZSTK474 is a novel, potent and ATP-competitive pan-PI3K inhibitor (class I) with potential anticancer activity. |
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V69237 | α-Linolenic acid-13C18 (α-linolenic acid 13C18) | 287111-28-8 | α-Linolenic acid-13C18 is 13C (carbon 13) labelled α-Linolenic acid. |
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V69230 | α-Linolenic acid-d14 (α-linolenic acid d14) | 1622944-40-4 | α-Linolenic acid-d14 is the deuterated form of α-Linolenic acid. |
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V69219 | α-Linolenic acid-d5 (α-linolenic acid d5) | 145191-04-4 | α-Linolenic acid-d5 is the deuterated form of α-Linolenic acid. |
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V1988 | Quercetin Dihydrate | 6151-25-3 | Quercetin, a naturally occuring polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. |
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V37833 | α-Linolenic acid | 463-40-1 | α-Linolenic acid is extracted from perilla and is an essential fatty acid that cannot be synthesized by the human body. |
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V4531 | Taselisib (GDC0032) | 1282512-48-4 | Taselisib (formerly also known as GDC-0032 or RG-7606), an imidazobenzoxazepin compound, is a novel and potent β-sparing small molecule inhibitor ofPI3KwithKivalues of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively. |
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V4528 | Inavolisib (GDC-0077) | 2060571-02-8 | Inavolisib (RG6114;GDC0077), extracted from patent WO 2017001645 A1, formula I, is a novel, potent and orally bioavailablePI3Kinhibitor with potential anticancer activity. |
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V3942 | Eganelisib (IPI-549) | 1693758-51-8 | Eganelisib (IPI 549;IPI549; IPI-549) is a novel, potent and selectivesmall molecule PI3Kγ (phosphoinositide-3-kinase)inhibitor with potential anticancer and immunomodulatory activity. |
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V0102 | Pictilisib (GDC0941, RG7321, GNE0941) | 957054-30-7 | Pictilisib (also called GDC-0941, Pictrelisib, RG-7321 and GNE-0941) is a potent and orally bioavailable inhibitor of PI3Kα/δ (class I phosphatidylinositol 3 kinase) with IC50 of 3 nM in cell-free assays. |
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V3825 | Pictilisib (GDC-0941) dimesylate | 957054-33-0 | Pictilisib dimesylate (also called GDC-0941 mesylate, Pictrelisib, RG7321 and GNE0941 mesylate) is a potent and orally available inhibitor of PI3Kα/δ (class I phosphatidylinositol 3 kinase) with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
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V0150 | Pilaralisib (XL147; SAR245408) | 934526-89-3 | Pilaralisib (formerly XL-147; SAR-245408) is a novel, potent, orally bioavailable, ATP-competitive, selective and reversible inhibitor of class I PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity. |