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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 and selective inhibitor of PI3Kα (IC50=0.038 nM). Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib 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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  • Duvelisib
    T19881201438-56-3In house
    Duvelisib (INK1197) is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.
    • $40
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  • 3-Methyladenine
    T18795142-23-4
    3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50=60 μM) and class III VPS34 (IC50=25 μM). 3-Methyladenine inhibits autophagy.
    • $35
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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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  • Alpelisib
    T19211217486-61-7
    Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity. Alpelisib inhibits PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib has antitumor activity and is targeted to PIK3CA mutant tumors.
    • $50
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  • Erucic acid
    T4867112-86-7
    Increased levels of erucic acid (22:1n9) have been found in the red blood cell membranes of autistic subjects with developmental regression (PMID: 16581239 ). Erucic acid (13(Z)-Docosenoic Acid) is broken down long-chain acyl-coenzyme A (CoA) dehydrogenase, which is produced in the liver. This enzyme breaks this long chain fatty acid into shorter-chain fatty acids. human infants have relatively low amounts of this enzyme and because of this, babies should not be given foods high in erucic acid. Erucic acid is found to be associated with isovaleric acidemia, which is an inborn error of metabolism.
    • $45
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  • Sophocarpine monohydrate
    T2746145572-44-7
    Sophocarpine monohydrate, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
    • $50
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  • Myricetin
    T0579529-44-2
    Myricetin (Cannabiscetin) is a naturally-occurring flavonoid found in many grapes, berries, fruits, vegetables, herbs, as well as other plants. Walnuts are a rich dietary source. It has been shown that myricetin has antioxidant properties.
    • $30
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  • Apilimod mesylate
    T3533870087-36-8
    Apilimod mesylate (STA 5326 mesylate) is a potent IL-12/IL-23 inhibitor.
    • $55
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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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  • 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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  • Glaucocalyxin A
    T4S049879498-31-0
    1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.
    • $100
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  • Quercetin Dihydrate
    T66306151-25-3
    Quercetin Dihydrate (Sophoretin) is a polyphenolic flavonoid that was found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine. It is used for their nervous system and anticancer effects.
    • $46
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  • Desmethyl-VS-5584
    T41991246535-95-4
    Desmethyl-VS-5584 is a dimethyl analog of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
    • $54
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  • PI3K-IN-38
    T616181382979-64-7
    PI3K-IN-38 is an orally available and potent PI3K inhibitor with an IC50 value of 0.541 µM for PI3K-α. PI3K-IN-38 exhibits anticancer and anti-inflammatory activity and inhibits tumor growth in vivo.
    • $195
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  • Torbafylline
    T67965105102-21-4In house
    Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.
    • $130
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  • mTOR inhibitor 9f
    T677011144075-42-2In house
    mTOR inhibitor 9f is a selective mTOR inhibitor with IC50 of 1.25nM and 82nM for mTOR and PI3Kα, respectively.
    • $197
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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.
    • $329
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  • TGX-115
    T24873351071-62-0In house
    TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β/p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.
    • $350
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  • PIK-inhibitors
    T3190371934-59-7
    PIK-inhibitors (MDK34597) is a pan PI3K inhibitors, an analog of PI-103.
    • $59
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  • PI3Kδ-IN-3
    T262521431540-99-6
    PI3Kδ-IN-3 (TC KHNS 11) is a PI3Kδ inhibitor with an IC50 value of 9 nM.PI3Kδ-IN-3 has a favorable pharmacokinetic profile and inhibits B cell function.
    • $86
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  • mTOR inhibitor 9d
    T677021144075-38-6In house
    mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.
    • $350
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  • GSK2292767 FA
    T6850L In house
    GSK2292767 FA is a potent and selective inhibitor of PI3Kδ (pIC50 : 10.1).GSK2292767 FA is more than 500-fold more selective than other PI3K isoforms.GSK2292767 FA can be used in the study of respiratory diseases.
    • $157
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  • IHMT-PI3Kδ-372 S-isomer
    T601962429889-61-0
    IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.
    • $117
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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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  • Safingol hydrochloride
    T83978139755-79-6In house
    Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) is a specific inhibitor of protein kinase C. It induces autophagy in solid tumor cells and cancer cell death by inhibiting the PKC and PI3-kinase pathways.BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor. Safingol hydrochloride inhibits PKC and PI3k.
    • $195 TargetMol
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  • PI3Kδ-IN-16
    T776672766437-35-6
    PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.
    • $195
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  • mTOR inhibitor 9e
    T677041144075-40-0In house
    mTOR inhibitor 9e is a selective mTOR inhibitor with IC50 of 0.68nM and 1359nM for mTOR and PI3Kα, respectively.
    • $329
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  • LY-294002 hydrochloride
    T4079934389-88-5
    LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα δ β (IC50: 0.5 0.57 0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.
    • $37
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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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  • SN32976
    T97881246202-11-8
    SN32976 is a pan PI3K inhibitor. SN32976 potently inhibited PI3K isoforms and mTOR, displaying preferential activity for PI3Kα and sparing of PI3Kδ.
    • $195
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  • PI3Kα/mTOR-IN-1
    T125891013098-90-2In house
    PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR. PI3Kα/mTOR-IN-1 shows 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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  • mTOR inhibitor 9c
    T677061144075-36-4In house
    mTOR inhibitor 9c is a selective mTOR inhibitor with IC50 of 0.7nM and 825nM for mTOR and PI3Kα, respectively.
    • $329
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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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  • Protectin D1
    T37379660430-03-5In house
    Protectin D1 (Neuroprotectin D1) is a neuroprotectin produced by neuronal cells and is a potential cardioprotective agent.Protectin D1 attenuates myocardial ischemia/reperfusion injury and inhibits imiquimod-induced psoriasis-like skin inflammation by modulating the PI3K/AKT signaling pathway.
    • $245
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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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  • 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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  • MSC2360844
    T121151305267-37-1In house
    MSC2360844 is a potent, orally active and selective inhibitor of PI3Kδ(IC50 of 145 nM).
    • $80
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  • PI3K/Akt/mTOR-IN-2
    T605642757804-89-8In house
    PI3K Akt mTOR-IN-2 is a potent PI3K AKT mTOR inhibitor.PI3K Akt mTOR-IN-2 has anticancer effects and is selective for MDA-MB-231 cells with an IC50 of 2.29 μM.PI3K Akt mTOR-IN-2 exhibits anticancer activity and induces cycle arrest and apoptosis in cancer cells. PI3K Akt mTOR-IN-2 has anticancer activity and can induce cycle arrest and apoptosis in cancer cells.
    • $33
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  • PKI-402
    T36561173204-81-3In house
    PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.
    • $30
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  • GDC-0349
    T65101207360-89-1In house
    GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
    • $33
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  • SAR-260301
    T168411260612-13-2In house
    SAR-260301 is an orally available and selective inhibitor of PI3Kβ (IC50: 23 nM).
    • $44
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  • WAY-600
    T67301062159-35-6In house
    WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1 P-S6K(T389) and mTORC2 P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
    • $32
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  • GSK2292767
    T68501254036-66-2In house
    GSK2292767 is a potent and selective PI3Kδ inhibitor.This compound is unstable in powder form and other related salt forms are recommended.
    • $110
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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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  • 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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  • Nemiralisib
    T154311254036-71-9In house
    Nemiralisib(GSK-2269557 free base) is an orally available, potent and specific PI3Kδ inhibitor with a pKi of 9.9.Nemiralisib is used for the treatment of respiratory diseases including chronic obstructive pulmonary disease.
    • $40
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  • PF-04979064
    T73431220699-06-8In house
    PF-04979064 is a potent and selective PI3K and mTOR dual kinase inhibitor(Ki of 0.13 nM and 1.42 nM,respectively).
    • $31
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  • BGT226
    T6072L915020-55-2In house
    BGT226 (NVP-BGT226) is a novel dual PI3K mTOR inhibitor, it acts on PI3K α β γ with IC50 of 4 nM 63 nM 38 nM, respectively.
    • $48
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  • hSMG-1 inhibitor 11j
    T88841402452-15-6
    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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