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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.

Inavolisib
T153752060571-02-8
Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.
  • $80
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Alpelisib
T19211217486-61-7
Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ γ δ with low activity (IC50=250 290 1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.
  • $50
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RLY-2608
T812642733573-94-7In house
RLY-2608 is a selective mutant PI3Kα inhibitor that inhibits tumor growth in a PIK3CA mutant xenograft model.
  • $538
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STX-478
T782112883540-92-7
STX-478 is an orally active and selective PI3Kα inhibitor that penetrates the blood-brain barrier and has anticancer activity to inhibit tumor growth.STX-478 is indicated for the study of breast cancer and other cancers.
  • $338
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LY294002
T2008154447-36-6
LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5 0.57 0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.
  • $34
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740 Y-P
TQ00031236188-16-1
740 Y-P (740YPDGFR) is a potent and cell-permeable activator of PI3K.
  • $89
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Myricetin
T0579529-44-2
Myricetin (Cannabiscetin) is a natural flavonoid and MEK1 inhibitor. Myricetin has hypoglycemic, antioxidant, hepatoprotective, anti-tumor and anti-inflammatory activities.
  • $30
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hSMG-1 inhibitor 11j
T88841402452-15-6In house
hSMG-1 inhibitor 11j is a pyrimidine derivative. hSMG-1 inhibitor 11j is a potent and selective inhibitor of hSMG-1, IC50 = 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα γ (IC50=92 60 nM) and CDK1 CDK2 (IC50=32 7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer.
  • $163 TargetMol
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Quercetin
T2174117-39-5
Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.
  • $42
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Wortmannin
T628319545-26-7
Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.
  • $32
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GSK251
T395732125968-05-8
GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.
  • $166
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iMDK
T9460881970-80-5In house
iMDK quarterhydrate is a potent PI3K inhibitor that inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate synergistically inhibits non-small cell lung cancer (NSCLC) with MEK inhibitors without harming normal cells and mice.
  • $54
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Fimepinostat
T20781339928-25-4
Fimepinostat (CUDC 907) is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types.
  • $39
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Torin 1
T60451222998-36-8
Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
  • $30
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GSK2636771
T20731372540-25-4
GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm.
  • $36
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Duvelisib (R enantiomer) hydrochloride
T11129L In house
Duvelisib (R enantiomer) hydrochloride (INK1197 R enantiomer HCl) is a PI3K inhibitor. Duvelisib (R enantiomer) hydrochloride is the less active enantiomer of Duvelisib.
  • $329
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MOMIPP
T334671363421-46-8
MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2].
  • $116
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740 Y-P acetate
TQ0003L1
740 Y-P acetate (740YPDGFR acetate) is a potent and cell-permeable PI3K activator.740 Y-P acetate tends to bind to GST fusion proteins containing the N- and C-terminal SH2 structural domains of p85, but not to GST alone.
  • $95
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PI3Kα/mTOR-IN-1
T125891013098-90-2In house
PI3Kα mTOR-IN-1 is a potent dual inhibitor of PI3Kα mTOR, with an IC50 of 7 nM for PI3Kα in a cell assay and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα [in a cell-free assay], respectively.
  • $656
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Taurocholic acid
TN225981-24-3
Taurocholic acid (N-Choloyltaurine) is a bile acid involved in the emulsification of fats.Taurocholic acid is cytoprotective, preventing tumor necrosis factor-alpha-induced cholangiocyte damage via a PI3K-mediated pathway.
  • $55
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GNE-477
T36921032754-81-6
GNE-477 is a potent and efficacious dual (PI3K mTOR) inhibitor.
  • $64
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Isoprenaline hydrochloride
T105651-30-9
Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
  • $33
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Apilimod
T2018541550-19-0
Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.
  • $43
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Apilimod 2HCl
T68485870087-37-9
Apilimod 2HCl (STA 5326 2HCl) is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation, IL-1β secretion, and cellular pyroptosis, and is used in the study of amyotrophic lateral sclerosis.
  • $1,520
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Gedatolisib
T19701197160-78-3
Gedatolisib (PF-05212384) 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.
  • $45
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Recilisib
T13862334969-03-8
Recilisib (ON 01210) is a radioprotectant that activates AKT and PI3K activities in cells.
  • $38
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GS-9901
T154201640247-87-5In house
GS-9901 is a selective, orally active and potent PI3Kδ inhibitor (IC50: 1 nM) for the study of non-Hodgkin's lymphoma and chronic lymphocytic leukemia.
  • $84 TargetMol
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Jolkinolide B
T2S104037905-08-1
Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud. Jolkinolide B induces apoptosis in cancer cells. Jolkinolide B can be used for studies on preventing and treating osteolysis.
  • $60
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Sapanisertib
T18381224844-38-5
Sapanisertib (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 activity.
  • $34
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Copanlisib
T63221032568-63-0
Copanlisib (BAY 80-6946) is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. By inhibiting the PI3K signaling pathway, Copanlisib may impede tumor cell growth and survival in certain tumor populations. Dysregulated PI3K signaling, often linked to tumorigenesis, may also contribute to tumor resistance to various antineoplastic agents.
  • $32
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mTOR inhibitor 13
T93101144075-44-4In house
mTOR inhibitor 13 is a selective mTOR inhibitor with IC50 of 0.29nM and 119nM for mTOR and PI3Kα, respectively.
  • $197
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Omipalisib
T18611086062-66-9
Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
  • $57
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I-OMe-Tyrphostin AG 538
T115931094048-77-7In house
I-OMe-Tyrphostin AG 538 is a specific IGF-1R inhibitor and ATP-competitive inhibitor of PI5P4Kα (IC50: 1 µM).I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deficient PANC1 cells.
  • $51
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Deguelin
T6817522-17-8
Deguelin ((-)-Deguelin) is a PI3K AKT Inhibitor, which is a natural product isolated from plants in the Mundulea sericea family.
  • $44
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Eganelisib
T54321693758-51-8
Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)
  • $40
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Duvelisib
T19881201438-56-3In house
Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).
  • $40
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PQR514
T700581927857-55-3In house
PQR514 is a potent PI3K inhibitor with anticancer activity and inhibits cancer cell proliferation.
  • $333 TargetMol
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Idelalisib
T1894870281-82-6
Idelalisib (GS-1101) 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.
  • $30
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Copanlisib dihydrochloride
T149981402152-13-9
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.
  • $47
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Momordin Ic
T341096990-18-0
Momordin Ic (Momordin 1c) might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MAPK and PI3K-mediated iNOS and HO-1 pathways. Also, Momordin Ic accelerates gastrointestinal transit partially by stimulating synthesis of 5-HT to act through 5-HT(2), which, in turn, increases synthesis of prostaglandins.
  • $30
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1-Deoxynojirimycin
T367519130-96-2
1-Deoxynojirimycin (Moranoline) is a potent α-glucosidase inhibitor, suppressing postprandial blood glucose, thereby possibly preventing diabetes mellitus.
  • $38
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Isorhamnetin
T2836480-19-3
Isorhamnetin (3-methylquercetin) is the methylated metabolite of quercetin. Quercetin is an important dietary flavonoid with in vitro antioxidant activity. Isorhamnetin prevents endothelial cell injuries from oxidized LDL via inhibition of lectin-like ox-LDL receptor-1 upregulation, interference of ox-LDL-mediated intracellular signaling pathway (p38MAPK activation, NF-kappaB nuclear translocation, eNOS expression) and the antioxidant activity of isorhamnetin. Isorhamnetin prevents endothelial dysfunction, superoxide production, and overexpression of p47phox induced by angiotensin II. Isorhamnetin appears to be a potent drug against esophageal cancer due to it's in vitro potential to not only inhibit proliferation but also induce apoptosis of Eca-109 cells.
  • $34
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Buparlisib
T1827944396-07-0
Buparlisib (BKM120) is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52 166 116 nM for p110α, p110β, and p110δ).
  • $57
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YS-49
T13376132836-42-1
YS-49 is an activator of PI3K Akt (a downstream target of RhoA).
  • $41
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KU-55933
T2685587871-26-9
KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.
  • $43
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AS-252424
T6208900515-16-4
AS-252424 is a potent and selective inhibitor of PI3Kγ with an IC50 of 33 nM and demonstrates over 10-fold selectivity for PI3Kγ versus PI3Kα.
  • $33
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PIK-75
T2667372196-67-3
PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
  • $38
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PI5P4Ks-IN-2
T720322766854-03-7In house
PI5P4Ks-IN-2 is an inhibitor of the phosphatidylinositol 5-phosphate 4-kinase PI5P4Kγ. Targeting the PI5P4K isoforms, PI5P4Ks-IN-2 inhibited PI5P4Kα, PI5P4Kβ, PI5P4Kγ, and PI5P4Kγ+, with IC50 values of <4.3, <4.6, 6.2, and 0.32, respectively.
  • $163
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