PI3K
PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is 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.
Products for PI3K
- Cat.No. Product Name Information
- GC13725 NVP-BAG956 A dual PDK1 and class I PI3K inhibitor
- GC16145 NVP-BGT226 BGT226 (NVP-NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.
- GC14504 NVP-BKM120 Hydrochloride An inhibitor of class I PI3K isoforms
- GC36786 NVP-QAV-572 NVP-QAV-572 is a PI3K inhibitor extracted from patent US7998990B2, Compound Example 8, has an IC50 of 10 nM.
- GC62141 NVS-PI3-4 NVS-PI3-4 is a specific PI3Kγ inhibitor.
- GC36807 ON 146040 ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
- GN10732 Oroxin B
- GC36832 P110δ-IN-1 P110δ-IN-1 is a potent and selective inhibitor of P110δ extracted from patent WO 2014055647 A1, with an IC50 of 8.4 nM.
- GC32916 Parsaclisib (INCB050465) Parsaclisib (INCB050465) (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib (INCB050465) shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib (INCB050465) can be used for the research of relapsed or refractory B-cell malignancies.
- GC62593 Parsaclisib hydrochloride Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies.
- GC16417 PF-04691502 PI3K/mTOR (FRAP) inhibitor
- GC19283 PF-04979064 PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
- GC15653 PF-05212384 (PKI-587) PF-05212384 (PKI-587) (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PF-05212384 (PKI-587) is equally effective in both complexes of mTOR, mTORC1 and mTORC2.
- GC62556 PF-06843195 PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
- GC12375 PF-4989216 Selective oral PI3K inhibitor
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GC10386
PI 828
PI 3-Kinase inhibitor
- GC11165 PI-103 Class I PI3K, mTOR and DNA-PK inhibitor
- GC16379 PI-103 Hydrochloride A potent, cell-permeable PI3K inhibitor
- GC15310 PI-3065 P110δkinase inhibitor
- GC38578 PI-828 A PI3K inhibitor
- GC62521 PI3Kα-IN-4 PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.
- GC36909 PI3Kα/mTOR-IN-1 PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
- GC36910 PI3Kγ inhibitor 1 PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
- GC36911 PI3kδ inhibitor 1 PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC50 of 3.8 nM.
- GC65199 PI3Kδ-IN-1 PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
- GC31751 PI3Kδ-IN-2 PI3Kδ-IN-2 (YY-20394) is a potent, orally bioavailable and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC50 of 6.4 nM.
- GC36907 PI3K-IN-2 PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively).
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GC69707
PI3K-IN-30
PI3K-IN-30 (compound 6d) is an effective PI3K inhibitor with IC50 values of 5.1 nM, 136 nM, 30.7 nM and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ respectively.
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GC69708
PI3K-IN-31
PI3K-IN-31 (Compound 6b) is an effective PI3K inhibitor with IC50 values of 3.7 nM, 74 nM, 14.6 nM and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ respectively. It has anti-cancer properties.
- GC67954 PI3K-IN-36
- GC36908 PI3K-IN-6 PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.
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GC69706
PI3K/AKT-IN-1
PI3K/AKT-IN-1 is an effective dual inhibitor of PI3K/AKT (with IC50 values of 6.99 μM, 4.01 μM, and 3.36 μM for PI3Kα, PI3Kδ, and AKT, respectively). It has anti-cancer activity by inhibiting the PI3K/AKT pathway and inducing caspase 3-dependent apoptosis.
- GC66463 PI3K/Akt/mTOR-IN-2 PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis.
- GC36905 PI3K/HDAC-IN-1 PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively.
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GC69709
PI3K/mTOR Inhibitor-11
PI3K/mTOR Inhibitor-11 is an orally active inhibitor of PI3K/mTOR (with IC50 values of 3.5, 4.6, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR, respectively). It regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 protein. PI3K/mTOR Inhibitor-11 can be used in cancer research.
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GC69710
PI3K/mTOR Inhibitor-13 sodium
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositide 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual disorders, solid tumors, and idiopathic pulmonary fibrosis (IPF).
- GC66447 PI3K/mTOR Inhibitor-4 PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.
- GC36906 PI3Kdelta inhibitor 1 PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
- GC32847 PI4KIIIbeta-IN-9 PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
- GC62340 PIK-108 PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
- GC15982 PIK-293 PI3K inhibitor
- GC13612 PIK-294 highly selective p110δ inhibitor
- GC16904 PIK-75 PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
- GC17199 PIK-90 PI3K inhibitor,potent selective
- GC13089 PIK-93 PI3Kγ/PI4KIIIβ/PI3Kα inhibitor
- GC14679 PIK-III PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM.
- GC36917 Pilaralisib A class I PI3K inhibitor
- GC62140 PKI-179 PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.
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GC17104
PKI-402
PI3K inhibitor,selective, reversible and ATP-competitive
- GN10312 Polygalasaponin F
- GC11003 PP121 Dual inhibitor of tyrosine and phosphoinositide kinases
- GC33385 PQR-530 A dual inhibitor of PI3Kα and mTOR
- GC19300 PQR309 PQR309 (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. PQR309 is an mTORC1 and mTORC2 inhibitor.
- GC12889 PX 866 PX 866 (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
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GN10266
Quercetin
Quercetin is an important dietary flavonoid, present in vegetables, fruits, seeds, nuts, tea and red wine.
- GC61227 Quercetin D5 Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
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GC15665
Quercetin dihydrate
PLA2 and PI 3-kinase inhibitor
- GC38401 rac-AZD 6482 rac-AZD 6482 ((Rac)-KIN-193) is the racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
- GC33130 Recilisib (Ex-RAD) Recilisib (Ex-RAD) (ON 01210) is a radioprotectant, which can activate AKT, PI3K activities in cells.
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GC12415
Rigosertib
PI3K/PLK1 inhibitor
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GC13580
Rigosertib sodium
Non-ATP-competitive inhibitor of PLK1
- GC14884 SAR245409 (XL765) SAR245409 (XL765) (XL-147 derivative 1) is a potent inhibitor of PI3K. SAR245409 (XL765) (25 μM) blocks PI3K/Akt signaling pathways.
- GC18479 SAR260301 SAR260301 is an inhibitor of phosphatidylinositol 3-kinase (PI3K) isoform β (IC50 = 52 nM).
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GC11471
SAR405
SAR405 is a Vps34 inhibitor (IC50=1.2 nM),SAR405 inhibits autophagy caused by mTOR inhibition.
- GC25913 Selective PI3Kδ Inhibitor 1 (compound 7n) Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
- GC31666 Seletalisib (UCB5857) Seletalisib (UCB5857) (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.
- GC37633 SF1126 SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis.
- GC19328 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
- GC60339 SKI V SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.
- GN10681 Sophocarpine
- GC64223 Sophocarpine monohydrate Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory.
- GC62456 SRX3207 SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
- GC62342 TASP0415914 TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM.
- GC50332 TC KHNS 11 Potent and selective PI 3-kinase δ inhibitor; orally bioavailable
- GC32828 Tenalisib (RP6530) Tenalisib (RP6530) (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
- GC15151 TG100-115 PI3Kγ/PI3Kδ inhibitor
- GC16231 TG100713 pan-PI3K inhibitor
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GC18164
UCB9608
PI4KIIIβ inhibitor
- GC19355 Umbralisib TGR-1202 is a PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively.
- GC37854 Umbralisib hydrochloride Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach.
- GC37855 Umbralisib R-enantiomer Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
- GC37922 Voxtalisib A dual inhibitor of PI3K and mTORC
- GC26044 VPS34 inhibitor 1 (Compound 19) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
- GC32932 Vps34-IN-2 Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43.
- GC10436 VPS34-IN1 Vps34 inhibitor
- GC17771 VS-5584 (SB2343) A selective PI3K/mTOR kinase inhibitor
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GC70138
Vulolisib
Vulolisib is an effective and orally active phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values of 0.2 nM, 168 nM, 90 nM, and 49 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively. It has anti-proliferative activity against cancer cells and also exhibits anti-tumor activity.
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GC12338
Wortmannin
Wortmannin is a highly potent direct inhibitor of PI3-kinase specificity originally derived from fungi (1,2).
- GC13321 WYE-687 MTOR inhibitor,ATP-competitive and selective
- GC38473 WYE-687 dihydrochloride WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
- GC12709 XL147 XL147 (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
- GC12336 XL765 PI3K/mTOR inhibitor
- GC64992 YH-306 YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization.
- GC10982 YM201636 PIKfyve inhibitor,potent and selective
- GC37954 YS-49 YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells.
- GC37955 YS-49 monohydrate YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells.
- GC62480 Zandelisib Zandelisib (ME-401) is a phosphatidylinositol 3-kinase (PI3K) inhibitor extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.
- GC19540 α-Linolenic Acid An essential fatty acid found in leafy green vegetables