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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V0126 | GSK1059615 | 958852-01-2 | GSK1059615 is a novel, potent and reversible inhibitor of P13K (phosphatidylinositol-3-kinases) with potential anticancer activity. |
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V2546 | GSK2292767 | 1254036-66-2 | GSK2292767 is a novel and selective PI3Kδ inhibitor being investigator for the treatment of respiratory diseases such as asthma and COPD. |
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V0135 | GSK2636771 | 1372540-25-4 | GSK2636771 is a novel, potent, selective and orally bioavailable inhibitor of PI3Kβ (phosphatidylinositol 3-kinase β)with potential anticancer activity. |
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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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V0148 | HS-173 | 1276110-06-5 | HS-173 is a novel and potent PI3Kα (phosphatidylinositol 3-kinase) inhibitor (IC50 = 0.8 nM) with a potential to be used asan effective therapeutic agent for ameliorating liver fibrosis. |
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V0110 | IC-87114 | 371242-69-2 | IC-87114 is a novel, potent, selective andATP-competitive PI3Kδ inhibitor (p110delta-selective) with potential anticancer activity. |
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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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V80354 | IHMT-PI3K-455 | IHMT-PI3K-455 (Compound 15u) is a specific and orally bioactive dual PI3Kγ/δ inhibitor. | |
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V76896 | iMDK quarterhydrate | iMDK quarterhydrate is a potent PI3K inhibitor that suppresses the growth factor MDK (also known as midkine or MK). | |
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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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V3109 | IPI-3063 | 1425043-73-7 | IPI-3063 is a potent and selective PI3Kp110δinhibitor with IC50 of 2.5 ± 1.2 nM and IC50 values of >1000 nM for other classes of PI3K isoforms (p110α, p110β, p110γ). |
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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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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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V0103 | LY294002 | 154447-36-6 | LY294002,a morpholine-containing compound designed based on the flavonoid quercetin,is apotent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively. |
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V69220 | MCX 28 | 1414453-58-9 | MCX 28 is a PI3K/mTOR/PIM inhibitor showing low nanomolar activity. |
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V25217 | ME-401 (P110δ-IN-1 ) | 1595129-71-7 | PWT143, formerly known as ME-401, is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic 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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V2898 | MLN-1117 | 1268454-23-4 | Serabelisib (formerly known as INK-1117, MLN-1117, and/or TAK-117) is a potent, selective, and oral bioavailable inhibitor of PI3Kα (phosphoinositide 3-kinase) isoform with IC50 of 21 nmol/L against PI3Kα. |
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V0217 | MLS-2052 (GSK-3 Inhibitor IX; BIO) | 667463-62-9 | MLS2052 (also known as BIO, GSK3 Inhibitor IX, 6-Bromoindirubin-3-oxime) is a novel, potent,cell-permeable bis-indolo and specific inhibitor of GSK-3 (glycogen synthase kinase-3) with potential antitumor activity. |
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V2539 | Nemiralisib (GSK2269557) | 1254036-71-9 | Nemiralisib (GSK-2269557) is a novel, potent and selective PI3Kδ inhibitor with pKi of 9.9. |
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