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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V2543 | Deguelin | 522-17-8 | Deguelin [(-)-Deguelin, (-)-cis-Deguelin], a naturally occurring rotenoid isolated from plants in the Mundulea sericea family, is an Akt inhibitor with anti-tumor effect on several cancers; it acts by decreasing levels of phosphorylated Akt. |
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V69206 | DS-7423 | 1222104-37-1 | DS-7423 is a dual (bifunctional) inhibitor of PI3K and mTOR, with IC50s of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively. |
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V0127 | Duvelisib (IPI-145, INK1197) | 1201438-56-3 | Duvelisib (formerly known as IPI-145 and INK1197, trade name: Copiktra), an isoquinolinone derivative, is a novel potent, orally bioactive and selective small-molecule phosphoinositide-3 kinases (PI3K) inhibitor with potential anticancer activity. |
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V3873 | Duvelisib R enantiomer | 1261590-48-0 | Duvelisib R enantiomer is the R-isomer of Duvelisib (formerly known as IPI-145 and INK1197, trade name:Copiktra) which is an isoquinolinone derivative and a novel potent, oral and selective small-molecule phosphoinositide-3 kinases (PI3K) inhibitor that selectively and potently inhibits two PI3K isoforms, PI3K-δ and PI3K-γ, with half maximal inhibition concentration IC50 of 2.5 nM and 27 nM respectively. |
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V20309 | Duvoglustat hydrochloride | 73285-50-4 | Duvoglustat hydrochloride (1-Deoxynojirimycin;AT-2220; Moranoline; deoxynojirimycin; DNJ) is a novel and potent alpha-glucosidase inhibitorfound in mulberry leaves and hasantihyperglycemic, anti-obesity, and antiviral activities. |
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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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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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V0132 | Fimepinostat (CUDC907) | 1339928-25-4 | Fimepinostat (also known as CUDC-907) is a potent, orally bioavailable, andsmall molecule dual inhibitor of PI3K and HDAC (PI3Kα and HDAC1/2/3/10) with potential anticancer activity. |
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V19873 | Fluorofenidone (AKF-PD; AKFPD) | 848353-85-5 | Fluorofenidone(AKF-PD; AKFPD),a derivative of AMR69, a promising multifunctional antifibrosis pyridinone drug whichact as a potent inhibitor of nicotinamide adeninedinucleotide phosphate oxidase via PI3K/Akt pathway in the pathogenesis of renal interstitial fibrosis. |
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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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V2541 | GDC-0084 (Paxalisib; RG7666) | 1382979-44-3 | GDC-0084 (Paxalisib; RG7666) is a novel, potent and brain penetrant inhibitor of phosphatidylinositol 3-kinase (PI3K) and mTOR with potential antineoplastic activity. |
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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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V0128 | Gedatolisib (PF05212384, PKI587) | 1197160-78-3 | Gedatolisib (also called PF-05212384, PKI-587) is a novel, highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with potential anticancer activity. |
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V70264 | Gilmelisib | 1845777-61-8 | 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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