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PI3K Signaling Pathway Map

PI3K Signaling Pathways

PI3K Products

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Catalog No. Product Name Information Product Use Citations Product Validations
E0020 Lupenone Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway.
E0121 Parsaclisib (INCB050465)

Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

E2366New IHMT-PI3Kδ-372 IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay.
E2375New PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
E2384New (E)-Akt inhibitor-IV (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic.
E2401New SPP-86 SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
E2823New PIK-108 PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
E3106New Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E3234New Trichosanthis Pericarpium Extract Trichosanthis Pericarpium Extract is extracted from Trichosanthis Pericarpium, which can protects cardiomyocytes from Hypoxia/Reoxygenation Injury by Regulating PI3K/Akt/NO Pathway.
E3410New Tripterygium wilfordii Extract Tripterygium wilfordii Extract is extracted from Tripterygium wilfordii, the effective constituent of which can induce autophagy via inhibition of the PI3K/AKT/mTOR signaling pathway.
E3656New Dichroa febrifuga Extract Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
Cell Death Discov, 2022, 8(1):48
S0947 Cafestol Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.2609.2021
Theranostics, 2022, 12(9):4348-4373
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Cancer Cell, 2022, S1535-6108(22)00312-9
Blood, 2022, blood.2021014304
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Sci Adv, 2022, 8(29):eabm8780
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.1397.2021
S1072 ZSTK474 ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Br J Haematol, 2022, 10.1111/bjh.18187
Int J Mol Sci, 2022, 23(8)4277
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
S1118 XL147 analogue XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1169 TGX-221 TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
Nat Commun, 2022, 13(1):182
Molecules, 2022, 27(9)2742
Biomed Res Int, 2022, 2022:8568528
S1187 PIK-90 PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.
Mol Imaging, 2021, 2021:5594514
Nat Commun, 2020, 8;11(1):2291
G3 (Bethesda), 2020, 4;10(5):1585-1597
S1205 PIK-75 HCl PIK-75 HCl is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
Cell Mol Life Sci, 2022, 79(7):367
Cancers (Basel), 2022, 14(6)1575
Am J Cancer Res, 2022, 12(3):1102-1115
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Nat Commun, 2022, 13(1):2136
Blood Cancer J, 2022, 12(3):39
Elife, 2022, 11e71256
S1268 IC-87114 IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.
Cell Death Discov, 2022, 8(1):197
J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R
Front Med (Lausanne), 2021, 8:713312
S1273 Amarogentin

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

S1352 TG100-115 TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.
Elife, 2021, 10e68544
Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
Exp Mol Med, 2020, 22
S1360 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
Am J Cancer Res, 2022, 12(3):1102-1115
BMC Cancer, 2020, 20(1):4
Cell Rep, 2019, 27(3):820-834
S1362 Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
Cancer Cell, 2022, 40(7):754-767.e6
Cancers (Basel), 2022, 14(6)1575
Environ Mol Mutagen, 2022, 63(3):151-161
S1410 AS-605240 AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively.
Front Mol Neurosci, 2022, 15:881933
Brain Sci, 2022, 12(5)571
Int J Mol Sci, 2021, 22(23)12673
S1462 AZD6482 AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.
Cancer Diagn Progn, 2022, 2(3):391-404
Cancer Cell Int, 2021, 21(1):24
Cancer Cell, 2020, S1535-6108(20)30427-X
S1523 Voxtalisib (XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Cell Oncol (Dordr), 2020, 8
Cell Rep, 2015, 11(3):446-59
Mol Cancer Res, 2014, 12(5):703-13
S2207 PIK-293 PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively.
S2226 Idelalisib Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Cancer Cell, 2022, S1535-6108(22)00312-9
Blood, 2022, blood.2021014304
Nat Commun, 2022, 13(1):182
S2227 PIK-294 PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively.
Cell Metab, 2019, 29(6):1400-1409
Mol Cell Biol, 2012, 32(12):2268-78
S2247 Buparlisib (BKM120) Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00005-8
Nat Commun, 2022, 13(1):2500
Elife, 2022, 11e73796
S2347 Quercetin Dihydrate Quercetin (Sophoretin), a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Nucleic Acids Res, 2021, gkab538
Front Immunol, 2021, 12:649285
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Hum Mol Genet, 2022, ddac116
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
S2628 Gedatolisib (PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
Front Oncol, 2022, 12:862806
Int J Mol Sci, 2022, 23(8)4277
Leuk Lymphoma, 2022, 63(2):404-415
S2636 A66 A66 is a potent and specific p110α inhibitor with IC50 of 32 nM in a cell-free assay, >100 fold selectivity for p110α over other class-I PI3K isoforms.
Mol Cancer Res, 2022, 20(2):280-292
Phytomedicine, 2022, 101:154116
Mol Biol Rep, 2022, 10.1007/s11033-021-07068-4
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Cell Metab, 2022, S1550-4131(21)00542-8
Mol Cell, 2022, S1097-2765(22)00393-8
Nucleic Acids Res, 2022, gkac375
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
Cell, 2022, S0092-8674(22)00472-X
Cancers (Basel), 2022, 14(6)1575
Int J Mol Sci, 2022, 23(8)4077
S2671 AS-252424 AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
Front Physiol, 2021, 12:717119
Toxicology, 2021, 454:152747
J Gerontol A Biol Sci Med Sci, 2020, glaa216
S2681 AS-604850 AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.
Cancer Lett, 2021, S0304-3835(21)00532-2
Front Med (Lausanne), 2021, 8:713312
Biomaterials, 2019, 194:57-72
S2682 CAY10505 CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.
Br J Haematol, 2014, 166(4):529-39
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Nat Commun, 2022, 13(1):2500
Theranostics, 2022, 12(4):1659-1682
Cancers (Basel), 2022, 14(6)1575
S2699 CH5132799 CH5132799 (MEN1611, PA799) inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1.
Biochimie, 2014, 105:182-91
Am J Transl Res, 2014, 6(5):471-493
S2739 PKI-402 PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.
Antioxidants (Basel), 2022, 11(3)461
Cells, 2021, 10(5)1261
Mol Cells, 2021, 44(1):50-62
S2743 PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2.
Cancers (Basel), 2022, 14(6)1575
Evid Based Complement Alternat Med, 2022, 2022:8110796
Cells, 2021, 10(5)1261
S2749 BGT226 (NVP-BGT226) maleate BGT226 (NVP-BGT226) maleate is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
Cancer Biol Ther, 2017, 18(10):816-826
Oncotarget, 2016, 7(34):55690-55703
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2022, 13(1):2111
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(7):110373
S2759 Fimepinostat (CUDC-907) CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.
Transl Oncol, 2022, 18:101362
Blood Cancer J, 2021, 11(6):111
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
S2767 3-Methyladenine (3-MA) 3-Methyladenine (3-MA, NSC 66389) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.
Bioact Mater, 2023, 19:690-702
Nature, 2022, 603(7899):159-165
Autophagy, 2022, 10.1080/15548627.2022.2055285
S2802 Copanlisib (BAY 80-6946) Copanlisib (BAY 80-6946) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.
Haematologica, 2022, 10.3324/haematol.2021.279957
Int J Cancer, 2022, 10.1002/ijc.33983
Genome Med, 2021, 13(1):146
S2814 Alpelisib (BYL719) Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.
Nat Commun, 2022, 13(1):2500
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Sci Adv, 2022, 8(2):eabh3375
S2870 TG100713 TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
Nat Commun, 2020, 11(1):3816
MedChemComm, 2013, 10.1039/c3md00301a
S2893 NU7026 NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
Sci Signal, 2022, 15(715):eabh2290
J Biol Chem, 2022, S0021-9258(22)00301-5
Nucleic Acids Res, 2021, gkab584
S3220 Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells.
Biomed Pharmacother, 2021, 143:112204
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Phytomedicine, 2022, 102:154182
S3241 Loureirin A Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation.
S3243New Zeaxanthin Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
S3296 Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3309 Solasodine Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21.
S3785 Notoginsenoside R1 Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S5818 acalisib (GS-9820) Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK.
S5978 Gallein Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain.
Elife, 2021, 10e71689
S6516 GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.
Front Pharmacol, 2021, 12:659511
S6517 GNE-493 GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
Cell Death Discov, 2022, 8(1):120
S6541 MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.
S7016 VS-5584 (SB2343) VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. Phase 1.
Eur J Pharmacol, 2021, 910:174446
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
J Pediatr Surg, 2020, S0022-3468(20)30786-7
S7018 CZC24832 CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ.
Front Physiol, 2022, 13:903164
Molecules, 2022, 27(9)2742
Autophagy, 2021, 1-19
S7028 Duvelisib (IPI-145) Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
Haematologica, 2022, 10.3324/haematol.2021.279957
J Cell Mol Med, 2022, 26(10):3068-3073
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
S7103 Taselisib (GDC 0032) Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cancer Res, 2022, 82(12):2269-2280
Mol Oncol, 2022, 16(5):1091-1118
S7335 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
S7356 HS-173 HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
Front Med (Lausanne), 2021, 8:713312
Eur J Pharm Sci, 2021, 166:105961
Front Physiol, 2021, 12:717119
S7623 PI-3065 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
Nucleic Acids Res, 2020, 26;gkaa431
Leukemia, 2019, 33(6):1427-1438
S7645 Pilaralisib (XL147) Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
Int J Mol Sci, 2022, 23(8)4277
Cell Death Dis, 2021, 12(8):713
Genome Med, 2020, 18;12(1):17
S7646 Voxtalisib (XL765) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Toxicol Appl Pharmacol, 2022, 437:115886
Front Immunol, 2021, 12:761326
Genome Med, 2020, 18;12(1):17
S7675 PF-4989216 PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
Mol Pharm, 2017, 14(7):2368-2377
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Autophagy, 2022, 1-15
Autophagy, 2022, 10.1080/15548627.2022.2065617
Cell Death Dis, 2022, 13(4):398
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
Nat Commun, 2022, 13(1):83
Cell Death Dis, 2022, 13(4):398
Sci Adv, 2021, 7(40):eabj2485
S7694 AZD8186 AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.
Cell Rep, 2022, 38(9):110448
Mol Cancer Ther, 2022, 21(1):170-183
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
S7798 GNE-317 GNE-317 is a potent, brain-penetrant PI3K inhibitor.
S7813 AMG319 AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
Front Med (Lausanne), 2021, 8:713312
Toxicology, 2021, 454:152747
Int Immunopharmacol, 2021, 95:107570
S7937 Nemiralisib Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
Cell Mol Life Sci, 2021, 10.1007/s00018-021-04009-z
Front Immunol, 2020, 11:606893
Small GTPases, 2020, 10.1080/21541248
S7938 GSK2292767 GSK2292767 is a potent and selective PI3Kδ inhibitor.
S7966 AZD8835 AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
Molecules, 2022, 27(9)2742
Molecules, 2019, 24(7)
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
Cancer Cell, 2022, S1535-6108(21)00662-0
J Cell Sci, 2022, jcs.259138
J Biol Chem, 2022, 298(8):102187
S8002 GSK2636771 GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.
Leukemia, 2022, 10.1038/s41375-022-01595-0
Cancer Res, 2021, canres.0955.2021
Front Oncol, 2020, 10;10:331
S8045 KU-0060648 KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.
Chembiochem, 2021, 22(12):2177-2181
Biomedicines, 2021, 9(5)579
Cell, 2019, 176(3):505-519
S8132 Deguelin Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.
Cell Death Dis, 2020, 11(2):143
Front Oncol, 2020, 10:624493
Oncotarget, 2020, 11(46):4224-4242
S8157 GDC-0326 GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.
Cancer Immunol Res, 2020, 8(12):1532-1541
Microb Cell, 2018, ;5(12):545-554
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR with Kiapp values of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005
S8194 umbralisib (TGR-1202) Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
Haematologica, 2022, 10.3324/haematol.2021.279957
Exp Hematol, 2021, S0301-472X(21)00089-8
Eur J Immunol, 2020, 8
S8322 Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
J Cell Mol Med, 2021, 25(12):5602-5614
S8330 Eganelisib (IPI-549) Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.
J Immunother Cancer, 2022, 10(2)e003564
Sci Signal, 2021, 14(714):eabj0057
Exp Mol Med, 2020, 22
S8456 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.
EMBO J, 2022, 10.15252/embj.2021109352
Cell Rep, 2021, 37(4):109899
Cell, 2020, S0092-8674(20)31394-5
S8560 Seletalisib (UCB-5857) Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold).
J Leukoc Biol, 2022, 10.1002/JLB.1A0821-413RR
S8581 Serabelisib (TAK-117) Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
Clin Rheumatol, 2021, 10.1007/s10067-021-05765-w
Cell, 2020, S0092-8674(20)31394-5
Nat Commun, 2020, 11(1):3521
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Nat Genet, 2021, 53(4):435-444
J Agric Food Chem, 2021, 69(40):11847-11855
J Steroid Biochem Mol Biol, 2021, 209:105826
S8668 Inavolisib (GDC-0077) Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.
Cancer Res, 2022, 82(12):2269-2280
S8672 Tenalisib (RP6530) Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
S8693 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].
S8738 Bimiralisib (PQR309) Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Haematologica, 2022, 10.3324/haematol.2021.279957
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cancer Cell Int, 2021, 21(1):24
S8752 leniolisib (CDZ 173) Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.
S8779 Parsaclisib (INCB050465) Hydrochloride Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
S8917 ME-401 ME-401 (P110δ-IN-1, PWT-143) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S9054 Pectolinarin Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
S9190 Oroxin B Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment.
Theranostics, 2022, 12(2):910-928
J Cancer, 2021, 12(7):2140-2150
A5047New PI3 Kinase p85 alpha Rabbit Recombinant mAb PI3 Kinase p85 alpha Rabbit Recombinant mAb detects endogenous levels of total PI 3 Kinase p85 alpha.
A5048 PI3 Kinase p55 gamma Rabbit Recombinant mAb

PI3 Kinase p55 gamma Antibody detects endogenous levels of total PI3 Kinase p55 gamma.

A5164 PI3 Kinase p110 beta Rabbit Recombinant mAb PI3 Kinase p110 beta Rabbit Recombinant mAb detects endogenous level of total PI3 Kinase p110 beta.
Exp Neurol, 2021, S0014-4886(21)00275-2
A5218 PI 3 Kinase p110 delta Rabbit Recombinant mAb PI 3 Kinase p110 delta Rabbit Recombinant mAb detects endogenous level of total PI3 Kinase p110 delt.
E0785New 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, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
E3017New Poria Cocos Extract Poria Cocos Extract is extracted from Poria cocos, which can stimulate aquaporin-3 via the PI3K/Akt/mTOR signaling pathway.
S3294 Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
S5383 Erucic acid Erucic acid (cis-13-docosenoic acid) is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel.
S7865 740 Y-P (PDGFR 740Y-P) 740 Y-P (PDGFR 740Y-P, 740YPDGFR) is cell-permeable phosphopeptide activator of PI3K.
Cell Death Dis, 2022, 13(4):332
Cancer Biol Ther, 2022, 23(1):211-224
Biochem Biophys Res Commun, 2022, 597:83-90
E2391New α-Linolenic acid α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties.
S4572 Homosalate Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways.
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
E0020 Lupenone Lupenone (Lup-20(29)-en-3-one, lupeone) is an isolated compound exhibiting anti-oxidative, anti-inflammation, and anti-diabetic activities. Lupenone can protect SH-SY5y cells against METH-induced neuronal apoptosis through the PI3K/Akt pathway.
E0121 Parsaclisib (INCB050465)

Parsaclisib (INCB050465, INCB-50465, IBI376) is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

E2366New IHMT-PI3Kδ-372 IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay.
E2375New PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
E2384New (E)-Akt inhibitor-IV (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic.
E2401New SPP-86 SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
E2823New PIK-108 PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
E3106New Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E3234New Trichosanthis Pericarpium Extract Trichosanthis Pericarpium Extract is extracted from Trichosanthis Pericarpium, which can protects cardiomyocytes from Hypoxia/Reoxygenation Injury by Regulating PI3K/Akt/NO Pathway.
E3410New Tripterygium wilfordii Extract Tripterygium wilfordii Extract is extracted from Tripterygium wilfordii, the effective constituent of which can induce autophagy via inhibition of the PI3K/AKT/mTOR signaling pathway.
E3656New Dichroa febrifuga Extract Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
S0817 SKI-V SKI V is a noncompetitive and potent inhibitor of non-lipid sphingosine kinase with IC50 of 2 μM for GST-hSK. SKI-V also inhibits PI3K with IC50 of 6 μM for hPI3k. SKI-V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P) and induces apoptosis with antitumor activity.
Cell Death Discov, 2022, 8(1):48
S0947 Cafestol Cafestol is a natural diterpenes extracted from coffee beans. Cafestol induces apoptosis and regulates a variety of inflammatory mediators to reduce inflammation. Cafestol inhibits PI3K/Akt pathway. Cafestol also can reduce the production of ROS in the leukemia cell line HL60.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.2609.2021
Theranostics, 2022, 12(9):4348-4373
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Cancer Cell, 2022, S1535-6108(22)00312-9
Blood, 2022, blood.2021014304
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
S1065 Pictilisib (GDC-0941) Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.
Sci Adv, 2022, 8(29):eabm8780
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancer Res, 2022, canres.1397.2021
S1072 ZSTK474 ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Br J Haematol, 2022, 10.1111/bjh.18187
Int J Mol Sci, 2022, 23(8)4277
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
S1118 XL147 analogue XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S1169 TGX-221 TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
Nat Commun, 2022, 13(1):182
Molecules, 2022, 27(9)2742
Biomed Res Int, 2022, 2022:8568528
S1187 PIK-90 PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.
Mol Imaging, 2021, 2021:5594514
Nat Commun, 2020, 8;11(1):2291
G3 (Bethesda), 2020, 4;10(5):1585-1597
S1205 PIK-75 HCl PIK-75 HCl is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
Cell Mol Life Sci, 2022, 79(7):367
Cancers (Basel), 2022, 14(6)1575
Am J Cancer Res, 2022, 12(3):1102-1115
S1219 YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). YM-201636 suppresses the growth of liver cancer via the induction of autophagy.
Nat Commun, 2022, 13(1):2136
Blood Cancer J, 2022, 12(3):39
Elife, 2022, 11e71256
S1268 IC-87114 IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.
Cell Death Discov, 2022, 8(1):197
J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R
Front Med (Lausanne), 2021, 8:713312
S1273 Amarogentin

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

S1352 TG100-115 TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2.
Elife, 2021, 10e68544
Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
Exp Mol Med, 2020, 22
S1360 GSK1059615 GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
Am J Cancer Res, 2022, 12(3):1102-1115
BMC Cancer, 2020, 20(1):4
Cell Rep, 2019, 27(3):820-834
S1362 Rigosertib (ON-01910) Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.
Cancer Cell, 2022, 40(7):754-767.e6
Cancers (Basel), 2022, 14(6)1575
Environ Mol Mutagen, 2022, 63(3):151-161
S1410 AS-605240 AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively.
Front Mol Neurosci, 2022, 15:881933
Brain Sci, 2022, 12(5)571
Int J Mol Sci, 2021, 22(23)12673
S1462 AZD6482 AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.
Cancer Diagn Progn, 2022, 2(3):391-404
Cancer Cell Int, 2021, 21(1):24
Cancer Cell, 2020, S1535-6108(20)30427-X
S1523 Voxtalisib (XL765) Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Cell Oncol (Dordr), 2020, 8
Cell Rep, 2015, 11(3):446-59
Mol Cancer Res, 2014, 12(5):703-13
S2207 PIK-293 PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively.
S2226 Idelalisib Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Cancer Cell, 2022, S1535-6108(22)00312-9
Blood, 2022, blood.2021014304
Nat Commun, 2022, 13(1):182
S2227 PIK-294 PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively.
Cell Metab, 2019, 29(6):1400-1409
Mol Cell Biol, 2012, 32(12):2268-78
S2247 Buparlisib (BKM120) Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
Cancer Cell, 2022, S1535-6108(22)00005-8
Nat Commun, 2022, 13(1):2500
Elife, 2022, 11e73796
S2347 Quercetin Dihydrate Quercetin (Sophoretin), a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Nucleic Acids Res, 2021, gkab538
Front Immunol, 2021, 12:649285
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Hum Mol Genet, 2022, ddac116
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
S2628 Gedatolisib (PKI-587) Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
Front Oncol, 2022, 12:862806
Int J Mol Sci, 2022, 23(8)4277
Leuk Lymphoma, 2022, 63(2):404-415
S2636 A66 A66 is a potent and specific p110α inhibitor with IC50 of 32 nM in a cell-free assay, >100 fold selectivity for p110α over other class-I PI3K isoforms.
Mol Cancer Res, 2022, 20(2):280-292
Phytomedicine, 2022, 101:154116
Mol Biol Rep, 2022, 10.1007/s11033-021-07068-4
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Cell Metab, 2022, S1550-4131(21)00542-8
Mol Cell, 2022, S1097-2765(22)00393-8
Nucleic Acids Res, 2022, gkac375
S2658 Omipalisib (GSK2126458) Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1.
Cell, 2022, S0092-8674(22)00472-X
Cancers (Basel), 2022, 14(6)1575
Int J Mol Sci, 2022, 23(8)4077
S2671 AS-252424 AS-252424 is a novel, potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
Front Physiol, 2021, 12:717119
Toxicology, 2021, 454:152747
J Gerontol A Biol Sci Med Sci, 2020, glaa216
S2681 AS-604850 AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.
Cancer Lett, 2021, S0304-3835(21)00532-2
Front Med (Lausanne), 2021, 8:713312
Biomaterials, 2019, 194:57-72
S2682 CAY10505 CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM.
Br J Haematol, 2014, 166(4):529-39
S2696 Apitolisib (GDC-0980) Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
Nat Commun, 2022, 13(1):2500
Theranostics, 2022, 12(4):1659-1682
Cancers (Basel), 2022, 14(6)1575
S2699 CH5132799 CH5132799 (MEN1611, PA799) inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1.
Biochimie, 2014, 105:182-91
Am J Transl Res, 2014, 6(5):471-493
S2739 PKI-402 PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.
Antioxidants (Basel), 2022, 11(3)461
Cells, 2021, 10(5)1261
Mol Cells, 2021, 44(1):50-62
S2743 PF-04691502 PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2.
Cancers (Basel), 2022, 14(6)1575
Evid Based Complement Alternat Med, 2022, 2022:8110796
Cells, 2021, 10(5)1261
S2749 BGT226 (NVP-BGT226) maleate BGT226 (NVP-BGT226) maleate is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC50 of 4 nM/63 nM/38 nM. Phase 1/2.
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
Cancer Biol Ther, 2017, 18(10):816-826
Oncotarget, 2016, 7(34):55690-55703
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2022, 13(1):2111
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(7):110373
S2759 Fimepinostat (CUDC-907) CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1.
Transl Oncol, 2022, 18:101362
Blood Cancer J, 2021, 11(6):111
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
S2767 3-Methyladenine (3-MA) 3-Methyladenine (3-MA, NSC 66389) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.
Bioact Mater, 2023, 19:690-702
Nature, 2022, 603(7899):159-165
Autophagy, 2022, 10.1080/15548627.2022.2055285
S2802 Copanlisib (BAY 80-6946) Copanlisib (BAY 80-6946) is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.
Haematologica, 2022, 10.3324/haematol.2021.279957
Int J Cancer, 2022, 10.1002/ijc.33983
Genome Med, 2021, 13(1):146
S2814 Alpelisib (BYL719) Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.
Nat Commun, 2022, 13(1):2500
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Sci Adv, 2022, 8(2):eabh3375
S2870 TG100713 TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
Nat Commun, 2020, 11(1):3816
MedChemComm, 2013, 10.1039/c3md00301a
S2893 NU7026 NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
Sci Signal, 2022, 15(715):eabh2290
J Biol Chem, 2022, S0021-9258(22)00301-5
Nucleic Acids Res, 2021, gkab584
S3220 Trigonelline Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells.
Biomed Pharmacother, 2021, 143:112204
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S3238 Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.
Phytomedicine, 2022, 102:154182
S3241 Loureirin A Loureirin A is a flavonoid extracted from the red resin of the herbs of Dracaena cochinchinensis, which is known as Dragon's Blood. Loureirin A inhibits platelet activation by an impairment of PI3K/Akt signaling. Loureirin A inhibits Akt phosphorylation.
S3243New Zeaxanthin Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
S3296 Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3309 Solasodine Solasodine (Purapuridine, Solancarpidine, Solasodin, Salasodine, Salasdine) is a poisonous alkaloid chemical compound that occurs in plants of the Solanaceae family. Solasodine reduces the mRNA level of matrix metalloproteinase-2 (MMP-2), MMP-9 and extracellular inducer of matrix metalloproteinase (EMMPRIN), but increases the expression of reversion-inducing cysteine-rich protein with kazal motifs (RECK). Solasodine downregulates oncogenic microRNA-21 (miR-21), which has been known to target RECK. Solasodine also reduces PI3K/Akt signaling pathways and downregulates expression of miR-21.
S3785 Notoginsenoside R1 Notoginsenoside R1 (Sanchinoside R1) is the main ingredient with cardiovascular activity in Panax notoginseng. It inhibits TNF-α-induced PAI-1 overexpression via extracellular signal-related kinases (ERK1/2) and phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) signaling pathways.
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
S5554 Lanatoside C Lanatoside C is a cardiac glycoside with antiviral and anti-tumor activity. Lanatoside C induces G2/M cell cycle arrest and induces autophagy and apoptosis via attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR signaling pathways.
S5818 acalisib (GS-9820) Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK.
S5978 Gallein Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain.
Elife, 2021, 10e71689
S6516 GNE-477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.
Front Pharmacol, 2021, 12:659511
S6517 GNE-493 GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
Cell Death Discov, 2022, 8(1):120
S6541 MTX-211 MTX-211 is a first-in-class dual inhibitor of PI3K and EGFR kinase.
S7016 VS-5584 (SB2343) VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. Phase 1.
Eur J Pharmacol, 2021, 910:174446
Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0
J Pediatr Surg, 2020, S0022-3468(20)30786-7
S7018 CZC24832 CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ.
Front Physiol, 2022, 13:903164
Molecules, 2022, 27(9)2742
Autophagy, 2021, 1-19
S7028 Duvelisib (IPI-145) Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
Haematologica, 2022, 10.3324/haematol.2021.279957
J Cell Mol Med, 2022, 26(10):3068-3073
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
S7103 Taselisib (GDC 0032) Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
Cancer Cell, 2022, S1535-6108(21)00662-0
Cancer Res, 2022, 82(12):2269-2280
Mol Oncol, 2022, 16(5):1091-1118
S7335 IPI-3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
S7356 HS-173 HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
Front Med (Lausanne), 2021, 8:713312
Eur J Pharm Sci, 2021, 166:105961
Front Physiol, 2021, 12:717119
S7623 PI-3065 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
Nucleic Acids Res, 2020, 26;gkaa431
Leukemia, 2019, 33(6):1427-1438
S7645 Pilaralisib (XL147) Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
Int J Mol Sci, 2022, 23(8)4277
Cell Death Dis, 2021, 12(8):713
Genome Med, 2020, 18;12(1):17
S7646 Voxtalisib (XL765) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
Toxicol Appl Pharmacol, 2022, 437:115886
Front Immunol, 2021, 12:761326
Genome Med, 2020, 18;12(1):17
S7675 PF-4989216 PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
Mol Pharm, 2017, 14(7):2368-2377
S7682 SAR405 SAR405 is a low-molecular-mass kinase inhibitor of PIK3C3/Vps34 (KD 1.5 nM) showing high selectivity and not be active up to 10 μM on class I and class II PI3Ks as well as on mTOR. SAR405 prevents autophagy and synergizes with MTOR (mechanistic target of rapamycin) inhibition in tumor cells.
Autophagy, 2022, 1-15
Autophagy, 2022, 10.1080/15548627.2022.2065617
Cell Death Dis, 2022, 13(4):398
S7683 PIK-III PIK-III (VPS34-IN2), which is a selective inhibitor of ​VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively.
Nat Commun, 2022, 13(1):83
Cell Death Dis, 2022, 13(4):398
Sci Adv, 2021, 7(40):eabj2485
S7694 AZD8186 AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.
Cell Rep, 2022, 38(9):110448
Mol Cancer Ther, 2022, 21(1):170-183
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
S7798 GNE-317 GNE-317 is a potent, brain-penetrant PI3K inhibitor.
S7813 AMG319 AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
Front Med (Lausanne), 2021, 8:713312
Toxicology, 2021, 454:152747
Int Immunopharmacol, 2021, 95:107570
S7937 Nemiralisib Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
Cell Mol Life Sci, 2021, 10.1007/s00018-021-04009-z
Front Immunol, 2020, 11:606893
Small GTPases, 2020, 10.1080/21541248
S7938 GSK2292767 GSK2292767 is a potent and selective PI3Kδ inhibitor.
S7966 AZD8835 AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
Molecules, 2022, 27(9)2742
Molecules, 2019, 24(7)
S7980 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
Cancer Cell, 2022, S1535-6108(21)00662-0
J Cell Sci, 2022, jcs.259138
J Biol Chem, 2022, 298(8):102187
S8002 GSK2636771 GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.
Leukemia, 2022, 10.1038/s41375-022-01595-0
Cancer Res, 2021, canres.0955.2021
Front Oncol, 2020, 10;10:331
S8045 KU-0060648 KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.
Chembiochem, 2021, 22(12):2177-2181
Biomedicines, 2021, 9(5)579
Cell, 2019, 176(3):505-519
S8132 Deguelin Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.
Cell Death Dis, 2020, 11(2):143
Front Oncol, 2020, 10:624493
Oncotarget, 2020, 11(46):4224-4242
S8157 GDC-0326 GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.
Cancer Immunol Res, 2020, 8(12):1532-1541
Microb Cell, 2018, ;5(12):545-554
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR with Kiapp values of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
Cell Stem Cell, 2019, 10.1016/j.stem.2019.10.005
S8194 umbralisib (TGR-1202) Umbralisib (TGR-1202, Rp-5264), a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively.
Haematologica, 2022, 10.3324/haematol.2021.279957
Exp Hematol, 2021, S0301-472X(21)00089-8
Eur J Immunol, 2020, 8
S8322 Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
J Cell Mol Med, 2021, 25(12):5602-5614
S8330 Eganelisib (IPI-549) Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.
J Immunother Cancer, 2022, 10(2)e003564
Sci Signal, 2021, 14(714):eabj0057
Exp Mol Med, 2020, 22
S8456 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.
EMBO J, 2022, 10.15252/embj.2021109352
Cell Rep, 2021, 37(4):109899
Cell, 2020, S0092-8674(20)31394-5
S8560 Seletalisib (UCB-5857) Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold).
J Leukoc Biol, 2022, 10.1002/JLB.1A0821-413RR
S8581 Serabelisib (TAK-117) Serabelisib (TAK-117, INK-1117, MLN-1117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
Clin Rheumatol, 2021, 10.1007/s10067-021-05765-w
Cell, 2020, S0092-8674(20)31394-5
Nat Commun, 2020, 11(1):3521
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
S8596 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay. The IC50 value for Vps34 is 19 nM in vitro.
Nat Genet, 2021, 53(4):435-444
J Agric Food Chem, 2021, 69(40):11847-11855
J Steroid Biochem Mol Biol, 2021, 209:105826
S8668 Inavolisib (GDC-0077) Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.
Cancer Res, 2022, 82(12):2269-2280
S8672 Tenalisib (RP6530) Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
S8693 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].
S8738 Bimiralisib (PQR309) Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Haematologica, 2022, 10.3324/haematol.2021.279957
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cancer Cell Int, 2021, 21(1):24
S8752 leniolisib (CDZ 173) Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.
S8779 Parsaclisib (INCB050465) Hydrochloride Parsaclisib (INCB050465, IBI376) Hydrochloride is a potent and highly selective PI3Kδ(PI3K delta) inhibitor with an IC50 of 1 nM at 1 mM ATP in biochemical assay and approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.
S8917 ME-401 ME-401 (P110δ-IN-1, PWT-143) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S9054 Pectolinarin Pectolinarin is a major compound in Cirsium setidens with anti-inflammatory activity. Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin induces apoptosis via inactivation of the PI3K/Akt pathway.
S9190 Oroxin B Oroxin B (Hypocretin-2), one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels are downregulated, while PTEN is upregulated after Oroxin B treatment.
Theranostics, 2022, 12(2):910-928
J Cancer, 2021, 12(7):2140-2150
A5047New PI3 Kinase p85 alpha Rabbit Recombinant mAb PI3 Kinase p85 alpha Rabbit Recombinant mAb detects endogenous levels of total PI 3 Kinase p85 alpha.
A5048 PI3 Kinase p55 gamma Rabbit Recombinant mAb

PI3 Kinase p55 gamma Antibody detects endogenous levels of total PI3 Kinase p55 gamma.

A5164 PI3 Kinase p110 beta Rabbit Recombinant mAb PI3 Kinase p110 beta Rabbit Recombinant mAb detects endogenous level of total PI3 Kinase p110 beta.
Exp Neurol, 2021, S0014-4886(21)00275-2
A5218 PI 3 Kinase p110 delta Rabbit Recombinant mAb PI 3 Kinase p110 delta Rabbit Recombinant mAb detects endogenous level of total PI3 Kinase p110 delt.
E0785New 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, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
E3017New Poria Cocos Extract Poria Cocos Extract is extracted from Poria cocos, which can stimulate aquaporin-3 via the PI3K/Akt/mTOR signaling pathway.
S3294 Demethyl-Coclaurine Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
S5383 Erucic acid Erucic acid (cis-13-docosenoic acid) is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel.
S7865 740 Y-P (PDGFR 740Y-P) 740 Y-P (PDGFR 740Y-P, 740YPDGFR) is cell-permeable phosphopeptide activator of PI3K.
Cell Death Dis, 2022, 13(4):332
Cancer Biol Ther, 2022, 23(1):211-224
Biochem Biophys Res Commun, 2022, 597:83-90
E2391New α-Linolenic acid α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties.
S4572 Homosalate Homosalate (HMS, Homomenthyl salicylate) is an organic ultraviolet filter used in most sunscreens but has been reported to be toxic to marine organisms. Homosalate aggravates the invasion of human trophoblast cells as well as regulates intracellular signaling pathways including PI3K/AKT and MAPK pathways.
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
E2366New IHMT-PI3Kδ-372 IHMT-PI3Kδ-372 is a potent and selective phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor with an IC50 of 14 nM in the biochemical assay.
E2375New PI3K/mTOR Inhibitor-2 PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with antitumor activity.
E2384New (E)-Akt inhibitor-IV (E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic.
E2401New SPP-86 SPP-86, a potent and selective cell permeable inhibitor of rearranged during transfection (RET) tyrosine kinase with an IC50 of 8 nM, inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
E2823New PIK-108 PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
E3106New Dioscoreae Nipponicae Rhizoma Extract Dioscoreae Nipponicae Rhizoma Extract is extracted from the rhizome of Dioscorea nipponica, of which the main component decreases the phosphorylation in IGF-1R, which in turn inhibits the phosphorylation and activation of PI3K-AKT and Rap1-MEK signaling pathways, promoting cell apoptosis and Graves’ disease remission.
E3234New Trichosanthis Pericarpium Extract Trichosanthis Pericarpium Extract is extracted from Trichosanthis Pericarpium, which can protects cardiomyocytes from Hypoxia/Reoxygenation Injury by Regulating PI3K/Akt/NO Pathway.
E3410New Tripterygium wilfordii Extract Tripterygium wilfordii Extract is extracted from Tripterygium wilfordii, the effective constituent of which can induce autophagy via inhibition of the PI3K/AKT/mTOR signaling pathway.
E3656New Dichroa febrifuga Extract Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
S3243New Zeaxanthin Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
A5047New PI3 Kinase p85 alpha Rabbit Recombinant mAb PI3 Kinase p85 alpha Rabbit Recombinant mAb detects endogenous levels of total PI 3 Kinase p85 alpha.
E0785New 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, inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1, also is an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
E3017New Poria Cocos Extract Poria Cocos Extract is extracted from Poria cocos, which can stimulate aquaporin-3 via the PI3K/Akt/mTOR signaling pathway.
E2391New α-Linolenic acid α-Linolenic acid, an essential fatty acid isolated from seed oils, affects the process of thrombotic through the modulation of PI3K/Akt signaling, and possesses the anti-arrhythmic properties.
Tags: PI3K inhibition | PI3K cancer | PI3K activation | PI3K signaling pathway | PI3 kinase pathway | PI3K activity | PI3K phosphorylation | PI3K assay | PI3K inhibitor cancer | PI3K inhibitor drugs | PI3K targets | PI3K inhibitors ic50 | PI3K inhibitors in clinical trials | PI3K inhibitor review