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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V29655 | Aurantio-obtusin | 67979-25-3 | Aurantio-obtusin is a novel and potent anthraquinone isolated fromSemen Cassiae. |
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V0124 | AZD-6482 (KIN-193) | 1173900-33-8 | AZD6482(KIN193) is a novel, potent, selective and ATP competitive PI3Kβ (phosphatidylinositol-3-kinase) inhibitor with potential anticancer activity. |
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V0152 | AZD8186 | 1627494-13-6 | AZD8186 (also known as AZD) is a novel, potent and selective inhibitor of PI3Kβ (phosphatidylinositol 3-kinase β) with potential anticancer activity. |
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V2544 | AZD8835 | 1620576-64-8 | AZD8835 is a novel, selective, and orally bioavailable inhibitor of the class I (PI3K) catalytic subunit alpha (PIK3CA) PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively with potential antineoplastic activity. |
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V4264 | BGT226 (NVP-BGT226) | 915020-55-2 | BGT226 (also known as NVP-BGT226) is a novel dual class PI3K(phosphatidylinositol 3-kinase)/mammalian target of rapamycin (mTOR) inhibitorwith IC50 of 4 nM/63 nM/38 nM. |
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V0131 | BGT226 (NVP-BGT226) | 1245537-68-1 | BGT226 maleate (also known as NVP-BGT226 maleate) is a novel and potent dual inhibitor of class I PI3K (phosphatidylinositol 3-kinase)/mammalian target of rapamycin (mTOR) with potential anticancer activity. |
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V2864 | Bimiralisib (PQR309) | 1225037-39-7 | Bimiralisib (also known asPQR-309; PI3K-IN-2)is an orally bioavailable,brain-penetrant, and balanced pan-inhibitor of PI3K/mTOR (phosphoinositide-3-kinase/mammalian target of rapamycin) with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. |
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V3763 | BKM120 HCl (Buparlisib) | 1312445-63-8 | BKM120 HCl(also known as NVP-BKM120, or Buparlisib), the hydrochloride salt ofBKM-120,is a selective and potent Pan-class I PI3K inhibitor with anticancer activity. |
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V17019 | Brevianamide F | 38136-70-8 | Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin extracted from Colletotrichum gloeosporioides with anti-bacterial effect. |
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V0105 | Buparlisib (BKM120, NVP-BKM120) | 944396-07-0 | BKM120 (also known as NVP-BKM120, or Buparlisib) is a selective,orally bioavailable and potent Pan-class I PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. |
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V0139 | CAY10505 | 1218777-13-9 | CAY10505, the dehydroxylated form of AS-252424, is a novel,potent and selective inhibitor ofPI3Kγ (phosphoinositide 3-kinase) with a potential toimprove hypertension-associated vascular endothelial dysfunction. |
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V0138 | CH5132799 | 1007207-67-1 | CH5132799 is a novel and potent class I PI3K (phosphoinositide 3-kinase) inhibitor with potential anticancer activity. |
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V18587 | CNX-1351 | 1276105-89-5 | CNX-1351 (CNX1351; CNX 1351) is a novel, potent, covalent and selective inhibitor of PI3Kα with anticancer activity. |
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V0136 | Copanlisib (BAY80-6946; Aliqopa) | 1032568-63-0 | Copanlisib (formerly BAY 80-6946; brand name: Aliqopa) is a potent, ATP-competitive and pan-class I PI3K (phosphoinositide 3-kinase) inhibitor with potential anticancer activity. |
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V3911 | COPANLISIB HCl | 1402152-13-9 | Copanlisib HCl (formerly BAY-806946;BAY 80-6946;Aliqopa), the hydrochloride salt ofCopanlisib, is a pan-class I PI3K (phosphoinositide 3-kinase) inhibitor approved in 2017 for the treatment of relapsed follicular lymphoma. |
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V69216 | CXJ-2 | 2919976-92-2 | CXJ-2 is a cyclic peptide that displays moderate affinity for elastin-derived peptide (EDP). |
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V2542 | CZ415 | 1429639-50-8 | CZ415 is a potent, cell-permeable (Kd app = 6.9 nM), and ATP-competitive mTOR inhibitor with high selectivity over any other kinase (IC50 = 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT) and very good pharmacokinetic properties which include moderate clearance and good oral bioavailability. |
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V0145 | CZC24832 | 1159824-67-5 | CZC24832 is a novel, potent and highly selectiveinhibitor of PI3Kγ (phosphoinostide 3-kinase γ)with apotential for treatment for inflammatory and autoimmune diseases (e. |
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V0101 | Dactolisib (BEZ235, NVP-BEZ 235) | 915019-65-7 | Dactolisib (formerly also known as NVP-BEZ235; BEZ235; BEZ-235) is a novel, potent and dual ATP-competitive inhibitor of PI3K (phosphatidylinositol 3-kinase) and mTOR for p110α/γ/δ/β and mTOR(p70S6K) with anticancer activity. |
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V4263 | Dactolisib tosylate | 1028385-32-1 | Dactolisib tosylate (formerly also known as NVP-BEZ235 tosylate and BEZ-235 tosylate) is an ATP-competitive and dual inhibitor of PI3K (phosphatidylinositol 3-kinase) and mTOR for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. |
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