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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V81138 | PI3Kδ-IN-14 | PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50= 0.8 nM, K d: 84.8 nM). | |
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V69194 | PI3Kδ-IN-15 | 870281-17-7 | PI3Kδ-IN-15 (compound 6b) is a selective PI3Kδ inhibitor (antagonist) with IC50 of 0.5 nM for p110δ. |
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V69229 | PI3Kδ-IN-16 | 2766437-35-6 | PI3Kδ-IN-16 is a potent and specific inhibitor of PI3Kδ. |
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V69240 | PI3Kδ-IN-17 | 2768181-63-9 | PI3Kδ-IN-17 (Compound S5) is a potent PI3Kδ inhibitor (antagonist) with IC50 of 2.82?nM. |
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V81139 | PI3Kδ-IN-18 | Se15 is a selective inhibitor of PI3Kδ with IC50 of less than 0.1nM. | |
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V69190 | PI3Kδ-IN-8 | 2101518-75-4 | PI3Kδ-IN-8 is a specific and orally bioactive PI3Kδ inhibitor (antagonist) with IC50 of 3.3 nM. |
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V69208 | PI3Kδ-IN-9 | 2135922-40-4 | PI3Kδ-IN-9 is a selective PI3Kδ inhibitor (antagonist) with IC50 of 3.8 nM. |
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V69225 | Pichromene (S14161) | 883046-50-2 | Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. |
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V3825 | Pictilisib (GDC-0941) mesylate | 957054-33-0 | Pictilisib mesylate (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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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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V0140 | PIK-293 (IC-87114) | 900185-01-5 | PIK-293 (IC87114), the parent compound of PIK-294, is a novel, potent, and the first isoform-selective PI3K (phosphatidylinositol 3-kinase) inhibitor with with potential anticancer activity. |
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V0133 | PIK-294 | 900185-02-6 | PIK-294 is a novel, potent and highly selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ (IC50 = 10 nM)with potential anticancer activity, showed 1000-, 49- and 16-fold less potency against PI3Kα/β/γ, respectively. |
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V0116 | PIK-75 HCl | 372196-77-5 | PIK-75 HCl, the hydrochloride salt ofPIK-75, is a novel, potent, selective and imidazopyridine-basedp110α inhibitor with potential anticancer activity and with IC50 of 5.8 nM, which is 200-fold more potent than p110β. |
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V0122 | PIK-90 | 677338-12-4 | PIK-90 is a novel and potent PI3Kα/γ/δ inhibitor with potential anticancer activity. |
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V0120 | PIK-93 | 593960-11-3 | PIK-93, aphenylthiazole analog,is a novel, potent, and selective PI4K (PI4KIIIβ) inhibitor with antiviral effects (antienterovirus activity). |
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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. |
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V0112 | Pilaralisib analog (XL147 analog, SAR245408 analog) | 956958-53-5 | Pilaralisib analog (XL-147 analog, SAR-245408) is novel, selective, potent, orally bioavailableand reversible small moleculeinhibitor of Class 1 PI3K (phosphatidylinositol 3 kinase) family of kinases with potential anticancer activity. |
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V81151 | PITCOIN4 | PITCOIN4 is a selective class IIPI3K-C2α inhibitor. | |
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V69187 | PKI-179 hydrochloride | 1463510-35-1 | PKI-179 HCl is a potent and orally bioactive dual PI3K/mTOR inhibitor (antagonist) with IC50s of 8 nM and 24 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. |
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V0141 | PKI-402 | 1173204-81-3 | PKI-402 is a novel, potent, dual and pan-inhibitor of PI3K/mTOR (phosphatidylinositol 3-kinase/mammalian target of rapamycin)with potential anticancer activity. |
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