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PI3K

PI3K

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.

PI3K related products

Structure Cat No. Product Name CAS No. Product Description
PI3Kα-IN-4 V70262 PI3Kα-IN-4 2322293-83-2 PI3Kα-IN-4 is a specific and orally bioactive PI3Kα inhibitor (antagonist) with IC50 of 1.8 nM.
PI3Kγ inhibitor 4 V69192 PI3Kγ inhibitor 4 1821038-80-5 PI3Kγ inhibitor 4 is a specific and orally bioactive PI3Kγ inhibitor (antagonist) with IC50 of 40 nM.
PI3Kγ inhibitor 5 V69234 PI3Kγ inhibitor 5 2566569-31-9 PI3Kγ inhibitor 5 is an inhibitor (blocker/antagonist) of phosphoinositide 3-kinase gamma (PI3Kγ) with IC50 of 34 nM.
PI3Kγ inhibitor 6 V69222 PI3Kγ inhibitor 6 900515-01-7 PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor.
PI3Kγ inhibitor 7 V69196 PI3Kγ inhibitor 7 2575863-25-9 PI3Kγ inhibitor 7 (compound 2) is a potent orally bioactive PI3Kγ inhibitor (antagonist) with IC50s of 4768, 878.1, 3.42, and 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively.
PI3Kδ-IN-12 V81137 PI3Kδ-IN-12 PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC50 = 5.8), with pKis of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively.
PI3Kδ-IN-13 V69232 PI3Kδ-IN-13 1686137-02-9 PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM).
PI3Kδ-IN-14 V81138 PI3Kδ-IN-14 PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC50= 0.8 nM, K d: 84.8 nM).
PI3Kδ-IN-15 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.
PI3Kδ-IN-16 V69229 PI3Kδ-IN-16 2766437-35-6 PI3Kδ-IN-16 is a potent and specific inhibitor of PI3Kδ.
PI3Kδ-IN-17 V69240 PI3Kδ-IN-17 2768181-63-9 PI3Kδ-IN-17 (Compound S5) is a potent PI3Kδ inhibitor (antagonist) with IC50 of 2.82?nM.
PI3Kδ-IN-18 V81139 PI3Kδ-IN-18 Se15 is a selective inhibitor of PI3Kδ with IC50 of less than 0.1nM.
PI3Kδ-IN-8 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.
PI3Kδ-IN-9 V69208 PI3Kδ-IN-9 2135922-40-4 PI3Kδ-IN-9 is a selective PI3Kδ inhibitor (antagonist) with IC50 of 3.8 nM.
Pichromene (S14161) V69225 Pichromene (S14161) 883046-50-2 Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor.
Pictilisib (GDC-0941) mesylate 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).
Pictilisib (GDC0941, RG7321, GNE0941)) 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.
PIK-293 (IC-87114) 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.
PIK-294 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.
PIK-75 HCl 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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