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1-[2-methyl-3-(trifluoromethyl)benzyl]-2-methyl-7-(morpholin-4-yl)-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
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1-[2-methyl-3-(trifluoromethyl)benzyl]-7-(morpholin-4-yl)-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
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1-[2-methyl-3-(trifluoromethyl)benzyl]-7-[(2R)-2-methylmorpholin-2-yl]-6,7-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one
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1-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]-3-[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]urea
dual catalytic subunit alpha isoform/mTOR kinase inhibitor, demonstrates inhibition of tumor cell growth in vitro and in vivo and causes suppression of the pathway specific biomarkers in the human MDA-361 cell line
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
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i.e. LY294002, treatment prevents interleukin-13-induced hyper-responsiveness
2-(6-aminopurin-9-ylmethyl)-5-methyl-3-O-tolyl-3H-quinazolin-4-one
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i.e.IC87114, selective for isoform p110delta. Treatment prevents interleukin-13-induced hyper-responsiveness
2-(difluoromethyl)-1-[4,6-di-(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole
lead compound for structure-activity study
2-(methylsulfanyl)-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
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2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(2methylmorpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
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2-methyl-3-[2-methyl-3-(trifluoromethyl)benzyl]-5-(morpholin-4-yl)[1,2,4]triazolo[1,5-a]pyrimidin-7(3H)-one
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2-[(6-amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
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i.e. IC87114, selectively inhibits isoform p110delta
3-(2-morpholino-6-(2-(pyridin-4-yl)ethylamino)pyrimidin-4-yl)phenol
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3-(2-morpholino-6-(pyridin-2-ylmethoxy)pyrimidin-4-yl)phenol
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3-(4-morpholino-6-(pyridin-2-yl)pyrimidin-2-yl)phenol
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3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one
i.e. CAL-101, highly selective and small molecule inhibitor of isoform PI3Kdelta. Inhibitor blocks constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis
3-[4-(4-morpholinyl)thieno(3,2-d)pyrimidin-2-yl]-phenol
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a p110 PI3K isoform selective inhibitor
3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol
among the compounds tested, treatment with 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol or 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol leads to the most efficient inhibition
3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol
among the compounds tested, treatment with 3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol or 3-[4-(morpholin-4-yl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenol leads to the most efficient inhibition
4-(2-((6-methoxypyridin-3-yl)amino)-5-((4-(methylsulfonyl)piperazin-1-yl)methyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine
not inhibitory to serine/threonine kinase mTOR; not inhibitory to serine/threonine kinase mTOR
4-[2-[(6-methoxypyridin-3-yl)amino]-5-phenylpyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
not inhibitory to serine/threonine kinase mTOR; not inhibitory to serine/threonine kinase mTOR
4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol
4-[5-(3,6-dihydro-2H-pyran-4-yl)-2-[(6-methoxypyridin-3-yl)amino]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
not inhibitory to serine/threonine kinase mTOR; not inhibitory to serine/threonine kinase mTOR
5-[2,2-difluoro-benzo(1,3)-dioxol-5-ylmethylene]-thiazolidine-2,4-dione
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a p110 PI3K isoform selective inhibitor
6-amino-2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-4-methoxy-1H-benzimidazole
inhibitory against all three class Ia PI 3-kinase enzymes, i.e. p110alpha, p110beta, and p110delta, and also displays significant potency against two mutant forms of the p110alpha isoform, H1047R and E545K. In an in vivo U87MG human glioblastoma tumor xenograftmodel in Rag1-/- mice, and at a dose of 50mg/kg given by intraperitoneal injection it dramatically reduces cancer growth by 81% compared to untreated controls
7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one
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i.e. TGX221, selectively inhibits isoform p110beta. Compound decreases secretion of vascular endothelial growth factor and interleukin-6 in nonasthmatic airway smooth muscle cells and lung fibroblasts
AS604850
PI3Kgamma inhibitor 2
Baicalin
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10 microM, 35.5% inhibition of isoform PI3Kalpha
BYL719
a p110alpha-specific inhibitor, BYL719 fails to display selective growth inhibition in p110alphahigh cells
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CAL-101
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a specific inhibitor of the PI3Kdelta isoform
CapG
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nuclear actin-regulatory protein
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GSK2636771
a p110beta-specific inhibitor
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HS173
a p110alpha-specific inhibitor
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luteolin
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1 microM, 75.8% inhibition of isoform PI3Kalpha
MLN1117
a p110alpha-specific inhibitor
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myricetin
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1 microM, almost complete inhibition of isoform PI3Kalpha
N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylidene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
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i.e.PIK75, selectively inhibits isoform p110alpha. In cells stimulated with transforming growth factor-beta and/or 10% fetal bovine serum, compound attenuates transforming growth factor-induced fibronectin deposition in all cell types tested and decreases secretion of vascular endothelial growth factor and interleukin-6 in nonasthmatic airway smooth muscle cells and lung fibroblasts. Compound decreases cell survival in transforming growth factor-stimulated asthmatic, but not nonasthmatic, airway smooth muscle cells
N-[2-(dimethylamino)ethyl]-N-methyl-4-[([4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]carbamoyl)amino]benzamide
dual catalytic subunit alpha isoform/mTOR kinase inhibitor, demonstrates inhibition of tumor cell growth in vitro and in vivo and causes suppression of the pathway specific biomarkers in the human MDA-361 cell line. Good in vivo efficacy in the MDA361 human breast tumor xenograft model
PI103
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suppressing phosphatidylinositol 3-kinase activity by inhibitors LY294002 and PI103 selectively reduces both the mRNA and protein levels of peroxisome proliferator-activated receptor gamma coactivator PGC-1beta but not PGC-1alpha. Reducing PGC-1b expression also leads to reduced mRNA expression levels of uncoupling protein 1, 2 and superoxide dismutase 2. Correspondingly, mitochondrial membrane potential and reactive oxygen species levels are increased
PIK75
p110alpha inhibitor PIK75 shows a strong cytotoxicity to all glioblastoma cell lines tested
quercetagetin
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1 microM, almost complete inhibition of isoform PI3Kalpha
TGX-221-R
R-enantiomer of inhibitor TGX-221, 100fold more potent as a PI3K-beta inhibitor than the S-enantiomer
YM024
a p110alpha-selective PI3K inhibitor
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ZSTK474
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a phosphatidylinositol 3-kinase inhibitor, inhibited phosphorylation of Ser65, Thr70 and Thr37/46 in 4E-BP1 by PI3K. Identification of the ZSTK474-sensitive phosphoproteins in A-549 cells, overview
[(4-[2-[(3-hydroxyphenyl)amino]-1H-benzimidazol-1-yl]-1,3,5-triazin-2-yl)amino]acetonitrile
lead compound for structure-based design of inhibitors, dual inhibitor of phosphatidylinositol 3-kinase and serine/threonine kinase mTOR; lead compound for structure-based design of inhibitors, dual inhibitor of phosphatidylinositol 3-kinase and serine/threonine kinase mTOR
[3-[4-morpholin-4-yl-7-(pyrrolidin-1-ylmethyl)-5H-pyrrolo-[3,2-d ]pyrimidin-2-yl]phenyl]methanol
selective for catalytic subunit alpha isoform
3-Methyladenine
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treatment in full medium for a prolonged period of time leads to marked increases of the autophagic markers in cells. The increase of autophagic markers is the result of enhanced autophagic flux. The autophagy promotion activity is due to its differential temporal effects on class I and class III PI3K enzymes. 3-Methyladenine blocks class I PI3K persistently, whereas its suppressive effect on class III PI3K is transient. Treatment with 3-methyladenine in full medium significantly reduces the level of phosphatidylinositol 3-phosphate, the product of class III PI3K, at early time points, but almost completely blocks the product of phosphatidylinositol 3,4,5-trisphosphate up to 9 h
3-Methyladenine
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treatment in full medium for a prolonged period of time leads to marked increases of the autophagic markers in cells. The increase of autophagic markers is the result of enhanced autophagic flux. The autophagy promotion activity is due to its differential temporal effects on class I and class III PI3K enzymes. 3-Methyladenine blocks class I PI3K persistently, whereas its suppressive effect on class III PI3K is transient. Treatment with 3-methyladenine in full medium significantly reduces the level of phosphatidylinositol 3-phosphate, the product of class III PI3K, at early time points, but almost completely blocks the product of phosphatidylinositol 3,4,5-trisphosphate up to 9 h
4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol
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i.e. PI103. Inhibitory to phosphatidylinositol 3-kinases, TORC1 and DNA protein kinase. PI103 potently inhibits proliferation and invasion of a wide variety of human cancer cells in vitro and shows biomarker modulation consistent with inhibition of phosphatidylinositide 3-kinase signaling
4-[4-(morpholin-4-yl)-5a,6-dihydro[1]benzofuro[3,2-d]pyrimidin-2-yl]phenol
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i.e. PI-103. In human leukemic cell lines and in primary blast cells from acute myelogenous leukemia patients, PI-103 inhibits constitutive and growth factor-induced PI3K/Akt and mTORC1 activation. PI-103 is essentially cytostatic for cell lines and induces cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis. PI-103 has additive proapoptotic effects with etoposide in blast cells and in immature leukemic cells. PI-103 does not induce apoptosis in normal CD34รพ cells and has moderate effects on their clonogenic and proliferative properties
AS605240
PI3Kgamma inhibitor 1
AS605240
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a specific PI3Kgamma inhibitor, significantly delays lethality in Plasmodium berghei-infected wild-type micer
IC-87114
p110delta-specific small molecule inhibitor
IC-87114
p110delta-specific small molecule inhibitor
IC87114
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a specific inhibitor of the PI3Kdelta isoform, inhibits AML proliferation and augments the effects of a topoisomerase 2 inhibitor
IC87114
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a selective PI3Kdelta inhibitor
idelalisib
5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]quinazolin-4(3H)-one, a PI3Kdelta inhibitor used to treat hematological malignancies. The inhibitor idelalisib is selective, noncovalent, reversible, and ATP-competitive. The compound binds reversibly and noncovalently to the p110delta subunit of the kinase, analysis of binding interactions that confer the potency and selectivity of idelalisib, overview. Idelalisib is a propeller-shaped inhibitor
idelalisib
CAL-101, a p110delta inhibitor
LY294002
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LY294002
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a PI3K-specific inhibitor
LY294002
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specific inhibitor
LY294002
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a quercetin analogue
LY294002
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suppressing phosphatidylinositol 3-kinase activity by inhibitors LY294002 and PI103 selectively reduces both the mRNA and protein levels of peroxisome proliferator-activated receptor gamma coactivator PGC-1beta but not PGC-1alpha. Reducing PGC-1b expression also leads to reduced mRNA expression levels of uncoupling protein 1, 2 and superoxide dismutase 2. Correspondingly, mitochondrial membrane potential and reactive oxygen species levels are increased
LY294002
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a PI3K-specific inhibitor
LY294002
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a specific #PI3K inhibitor
LY294002
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inhibits sperm-induced activation of the tyrosine kinase Src and a transient increase in the intracellular concentration of Ca2+ at fertilization. LY294002 also has an inhibitory effect on the Ca2+-dependent breakdown of the Mos protein kinase and cyclin B2 as well as dephosphorylation of mitogenactivated protein kinase
PI-103
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a dual PI3K/mTOR inhibitor and a small synthetic molecule of the pyridofuropyrimidine class. PI-103 induces caspase activation and is cytotoxic to all T-cell acute lymphoblastic leukemia cell lines affecting PI3K/Akt/mTOR signaling, mechanism, overview
PI-103
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shows increased efficacy in inhibiting the growth of glioma cells due to its activity against both the class I PI3Ks and the PIK family member mTor
PIK-75
p110alpha-specific small molecule inhibitor
PIK-75
a p110alpha-selective PI3K inhibitor
PIK-75
p110alpha-specific small molecule inhibitor; p110alpha-specific small molecule inhibitor
PIK-75
p110alpha-specific small molecule inhibitor
PX-866
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irreversible PI3K inhibitor, shows selectivity for the alpha, delta, and gamma class I PI3K isoforms, inhibits the beta isoform at higher concentrations, and shows decreased selectivity for mTor
PX-866
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a PI3K inhibitor, inhibits also the oncogenic K-ras-induced bronchioalveolar stem cell accumulation and tumor growth in vivo
quercetin
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1 microM, 54.1% inhibition of isoform PI3Kalpha
quercetin
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from red wine extract, quercetin and red wine polyphenol extract inhibit the phosphorylation of Akt in vivo and show inhibitory effects on TNF-alpha-induced upregulation of MMP-9 and on the migratory phenotype of JB6 P+ mouse epidermal, mediated by suppression of the phosphorylation of Akt and the transactivation of activator protein-1 and nuclear factor-kappaB. Red wine extract and quercetin suppress TNF-alpha-induced PI3K activity by binding specifically to PI3K
TGX-221
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a p110 PI3K isoform selective inhibitor
TGX-221
p110beta-specific small molecule inhibitor
TGX-221
a p110beta-specific inhibitor
TGX-221
p110beta-specific small molecule inhibitor
Wortmannin
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Wortmannin
in nanomolar range
Wortmannin
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member of a class of steroidal furanoids, shows equally potent activity against all the class I PI3K enzymes, has antiproliferative effect
Wortmannin
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treatment with wortmannin results in sustained reduction of phosphatidylinositol 3-phosphate and a transient effect on production of phosphatidylinositol 3,4,5-trisphosphate with recovery after 9 h
Wortmannin
a PI3K inhibitor
Wortmannin
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treatment prevents interleukin-13-induced hyper-responsiveness
Wortmannin
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treatment with wortmannin results in sustained reduction of phosphatidylinositol 3-phosphate and a transient effect on production of phosphatidylinositol 3,4,5-trisphosphate with recovery after 9 h
XL147
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targets only the class I PI3Ks
additional information
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inhibition of PIK3CA induces apoptosis in mantle cell lymphoma cell lines
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additional information
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cyclic stretch causes a sustained decrease in activation of PI3-kinase and inhibits wound healing
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additional information
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pan-PI3K inhibition and inhibition of only PI3Kdelta results in attenuated vascular leakage, tissue eosinophilia, airway mucus production, and AHR as well as release of cytokines, chemokines and adhesion molecules
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additional information
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inhibitory activity of eighteen flavonoids and deduction of their structure-activity relationships. The number of hydroxyl groups in the A and B rings might promote the activity, while loss of C2-C3 double bond might reduce the activity. The results indicate that the flavonoids seem to exhibit more potent activity on PI3Kalpha and delta isoforms compared with that on PI3Kbeta and gamma isoforms
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additional information
in its resting state, PI3Kapha is autoinhibited by the interaction of a loop of the helical domain of p110alpha with a groove in the nSH2 domain of p85alpha. Despite this inhibition, the enzyme has a significant basal activity
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additional information
blockade of PI3K lipid signaling by expression of the pleckstrin homology of Akt1
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additional information
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blockade of PI3K lipid signaling by expression of the pleckstrin homology of Akt1
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additional information
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a combination of INPP4B overexpression and rucaparib blocks the PI3K/AKT signal pathway
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additional information
p110alpha-specific inhibitors (PIK75, BYL719, MLN1117, and HS173) are significantly toxic to astrocytes. The p110beta inhibitor TGX-221 and GSK2636771 mitigate the proliferation of p110betahigh U87MG and SF295 cells while having no effect on p110betalow A172 and LN229 cells
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