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PI3K/Akt/mTOR signaling PI3K

PI3K

Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer.PI3Ks are a family of related intracellular signal transducer enzymes capable of phosphorylating the 3 position hydroxyl group of the inositol ring of phosphatidylinositol (PtdIns). The pathway, with oncogene PIK3CA and tumor suppressor PTEN, is implicated in the sensitivity of cancer tumors to insulin and IGF1, and in calorie restriction.
Cat No. product name
T0579 Myricetin Myricetin is a naturally-occurring flavonoid found in many grapes, berries, fruits, vegetables, herbs, as well as other plants. Walnuts are a rich dietary sourc...
T1056 Isoprenaline hydrochlorideHOT Isoproterenol is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
T1826 Voxtalisib Analogue Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ ,also inhibits DNA-PK and mTOR.
T1827 BuparlisibHOT Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).
T1838 INK 128 INK 128 is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activ...
T1859 AZD8055HOT AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
T1861 Omipalisib GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
T1879 3-MethyladenineHOT 3-Methyladenine (3-MA) is a selective PI3KV inhibitor, and the IC50s against ps34 and PI3Kγ were 25/60 μM in HeLa cells, respectively.
T1894 IdelalisibHOT Idelalisib is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ.
T1916 Apitolisib Apitolisib, an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in t...
T1921 AlpelisibHOT Alpelisib is an orally bioavailable PI3Kα inhibitor (IC50: 5 nM in a cell-free assay) with potential antineoplastic activity and minimal effect on PI3Kβ/γ/δ...
T1949 CZC24832 CZC24832 is a selective inhibitor of PI 3-kinase γ.
T1961 Vistusertib AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
T1970 Gedatolisib Gedatolisib is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.
T1988 Duvelisib Duvelisib is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) wi...
T1994 PictilisibHOT Pictilisib (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3/33/3/75 nM for p110α/β/δ/γ).
T1999 Taselisib Taselisib is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity...
T2008 LY294002HOT LY294002 is an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It also blocks autophagosome formation.
T2061 APY0201 APY0201 is a effective, highly specific, ATP-competitive PIKfyve inhibitor (IC50: 5.2 nM). It can interrupt the conversion of phosphatidylinositol 3-phosphate (...
T2073 GSK-2636771 GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and adva...
T2083 PI3065 PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
T2084 ETP46464 ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
T2174 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit, and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor.
T2235 DactolisibHOT Dactolisib is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
T2248 AS-605240 AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50/Ki: 87.8 nM).
T2256 CNX-1351 CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor.
T2287 PIK-75 hydrochloride PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inh...
T2297 PIK-294 PIK-294 is a excellently specific p110δ inhibitor(IC50=10 nM).
T2308 HS-173 HS-173 is an effective PI3Kα inhibitor (IC50: 0.8 nM).
T2357 GSK-1059615 GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
T2365 Pilaralisib Pilaralisib is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trial...
T2377 XL147 analogue XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
T2414 TorkinibHOT Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
T2418 A66 A66 is a specific and effective p110α inhibitor(IC50=32 nM).
T2433 NU7026 NU7026 is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR...
T2461 PIK-90 PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
T2616 PIK-93 PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
T2619 CH5132799 CH5132799 has been used in trials studying the treatment of Solid Tumors.
T2660 IC-87114 IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).
T2661 TGX-221 TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.
T2667 PIK75 PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
T2672 TG100-115 TG100-115 is a PI3Kγ/δ inhibitor (IC50: 83/235 nM), with fewer effects on PI3Kα/β.
T2682 Acalisib Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ.
T2685 KU55933 KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
T3153 Serabelisib MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
T3190 PIK-inhibitors PIK-inhibitors is a pan PI3K inhibitors,an analog of PI-103.
T3348 PIK-293 PIK-293 is a PI3K inhibitor, for PI3Kδ( IC50=0.24 μM), and less potent for PI3Kα/β/ γ.
T3351 CC-223 CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor...
T3410 Momordin Ic Momordin Ic might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MA...
T3541 CC-115 CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
Myricetin
T0579CAS 529-44-2
Myricetin is a naturally-occurring flavonoid found in many grapes, berries, fruits, vegetables, herbs, as well as other plants. Walnuts are a rich dietary sourc...
Isoprenaline hydrochloride HOT
T1056CAS 51-30-9
Isoproterenol is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
Voxtalisib Analogue
T1826CAS 1349796-36-6
Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ ,also inhibits DNA-PK and mTOR.
Buparlisib HOT
T1827CAS 944396-07-0
Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).
INK 128
T1838CAS 1224844-38-5
INK 128 is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activ...
AZD8055 HOT
T1859CAS 1009298-09-2
AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
Omipalisib
T1861CAS 1086062-66-9
GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
3-Methyladenine HOT
T1879CAS 5142-23-4
3-Methyladenine (3-MA) is a selective PI3KV inhibitor, and the IC50s against ps34 and PI3Kγ were 25/60 μM in HeLa cells, respectively.
Idelalisib HOT
T1894CAS 870281-82-6
Idelalisib is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ.
Apitolisib
T1916CAS 1032754-93-0
Apitolisib, an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in t...
Alpelisib HOT
T1921CAS 1217486-61-7
Alpelisib is an orally bioavailable PI3Kα inhibitor (IC50: 5 nM in a cell-free assay) with potential antineoplastic activity and minimal effect on PI3Kβ/γ/δ...
CZC24832
T1949CAS 1159824-67-5
CZC24832 is a selective inhibitor of PI 3-kinase γ.
Vistusertib
T1961CAS 1009298-59-2
AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
Gedatolisib
T1970CAS 1197160-78-3
Gedatolisib is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.
Duvelisib
T1988CAS 1201438-56-3
Duvelisib is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) wi...
Pictilisib HOT
T1994CAS 957054-30-7
Pictilisib (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3/33/3/75 nM for p110α/β/δ/γ).
Taselisib
T1999CAS 1282512-48-4
Taselisib is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity...
LY294002 HOT
T2008CAS 154447-36-6
LY294002 is an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It also blocks autophagosome formation.
APY0201
T2061CAS 1232221-74-7
APY0201 is a effective, highly specific, ATP-competitive PIKfyve inhibitor (IC50: 5.2 nM). It can interrupt the conversion of phosphatidylinositol 3-phosphate (...
GSK-2636771
T2073CAS 1372540-25-4
GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and adva...
PI3065
T2083CAS 955977-50-1
PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
ETP46464
T2084CAS 1345675-02-6
ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
Quercetin
T2174CAS 117-39-5
Quercetin, a natural flavonoid present in vegetables, fruit, and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor.
Dactolisib HOT
T2235CAS 915019-65-7
Dactolisib is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
AS-605240
T2248CAS 648450-29-7
AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50/Ki: 87.8 nM).
CNX-1351
T2256CAS 1276105-89-5
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor.
PIK-75 hydrochloride
T2287CAS 372196-77-5
PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inh...
PIK-294
T2297CAS 900185-02-6
PIK-294 is a excellently specific p110δ inhibitor(IC50=10 nM).
HS-173
T2308CAS 1276110-06-5
HS-173 is an effective PI3Kα inhibitor (IC50: 0.8 nM).
GSK-1059615
T2357CAS 958852-01-2
GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
Pilaralisib
T2365CAS 934526-89-3
Pilaralisib is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trial...
XL147 analogue
T2377CAS 956958-53-5
XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
Torkinib HOT
T2414CAS 1092351-67-1
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
A66
T2418CAS 1166227-08-2
A66 is a specific and effective p110α inhibitor(IC50=32 nM).
NU7026
T2433CAS 154447-35-5
NU7026 is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR...
PIK-90
T2461CAS 677338-12-4
PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
PIK-93
T2616CAS 593960-11-3
PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
CH5132799
T2619CAS 1007207-67-1
CH5132799 has been used in trials studying the treatment of Solid Tumors.
IC-87114
T2660CAS 371242-69-2
IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).
TGX-221
T2661CAS 663619-89-4
TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.
PIK75
T2667CAS 372196-67-3
PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
TG100-115
T2672CAS 677297-51-7
TG100-115 is a PI3Kγ/δ inhibitor (IC50: 83/235 nM), with fewer effects on PI3Kα/β.
Acalisib
T2682CAS 870281-34-8
Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ.
KU55933
T2685CAS 587871-26-9
KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
Serabelisib
T3153CAS 1268454-23-4
MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
PIK-inhibitors
T3190CAS 371934-59-7
PIK-inhibitors is a pan PI3K inhibitors,an analog of PI-103.
PIK-293
T3348CAS 900185-01-5
PIK-293 is a PI3K inhibitor, for PI3Kδ( IC50=0.24 μM), and less potent for PI3Kα/β/ γ.
CC-223
T3351CAS 1228013-30-6
CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor...
Momordin Ic
T3410CAS 96990-18-0
Momordin Ic might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MA...
CC-115
T3541CAS 1228013-15-7
CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).