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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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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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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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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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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V5059 | Linperlisib (YY-20394) | 1702816-75-8 | Linperlisib (YY20394; PI3Kδ-IN-2)is a novel, potent, orally bioavailable, and highly selective PI3Kδ inhibitor that was being investigated in a phase I trial for patients with relapse or refractory B-cell malignancies. |
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V0147 | Quercetin (Sophoretin; NSC 9221; Kvercetin) | 117-39-5 | Quercetin (Sophoretin; NSC-9221; Kvercetin) is a natural flavonoid isolated from various vegetables, fruits and wine. |
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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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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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V4575 | Homosalate | 118-56-9 | Homosalate is an organic chemical compound used in sunscreens and cosmetics as a UV filter to absorb ultraviolet radiation in the UVB range, thusprotecting the skin from sun damage. |
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V0106 | Voxtalisib (XL-765, SAR-245409) | 934493-76-2 | Voxtalisib (also known as SAR245409, XL765) is a potent, orally bioavailable small molecule and dual inhibitor of mTOR/PI3K (mammalian target of rapamycin/phosphatidylinositol 3 kinase) with anticancer activity. |
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V0119 | Voxtalisib Analog (SAR245409 Analog, XL765 Analog) | 1349796-36-6 | Voxtalisib analogue (also known as PI3K-IN-1, SAR-245409Analog, XL-765Analog), aVoxtalisib derivative,is a novel, potent and orally bioavailable dual inhibitor of mTOR/PI3K with potential anticancer activity. |
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V0111 | Wortmannin (SL-2052; KY-12420) | 19545-26-7 | Wortmannin (SL2052; KY12420),a steroid metabolite of the fungi Penicillium funiculosum, is the first described, potentselective and irreversible PI3K inhibitor with potential anticancer activity. |
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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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V2538 | Miransertib (ARQ 092) | 1313881-70-7 | Miransertib (formerly known as ARQ 092) is an orally bioavailable and selective allosteric inhibitor of AKT with IC50 values of 5.0 nM, 4.5 nM, 16 nM for AKT1, 2,and 3, respectively. |
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V0104 | Idelalisib (CAL101, Zydelig, GS1101) | 870281-82-6 | Idelalisib (CAL-101, GS-1101; trade name Zydelig), an approved anticancer drug, is a potent and selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; it has 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. |
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V3968 | LENIOLISIB | 1354690-24-6 | Leniolisib (formerly CDZ173; CDZ-173; Joenja)is a novel, potent and selective PI3K (phosphatidylinositol 3-kinase inhibitor) inhibitor with immunomodulatory effects. |
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V2545 | Samotolisib (LY3023414; GTPL8918) | 1386874-06-1 | Samotolisib (LY3023414; GTPL8918)is an orally bioactive, selective and ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK withIC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. |
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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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