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Catalog No.	Product Name	Information	Product Use Citations
E0020^New	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^New	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.
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.
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 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.	Sci Rep, 2022, 12(1):241 Curr Res Pharmacol Drug Discov, 2022, 3:100076 Nat Commun, 2021, 12(1):7268
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.	Adv Healthc Mater, 2021, e2101944 Cell Chem Biol, 2021, S2451-9456(21)00254-3 Neurobiol Dis, 2021, 156:105407
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.	Nat Commun, 2022, 13(1):245 Cancer Cell, 2021, S1535-6108(21)00383-4 Cancer Cell, 2021, S1535-6108(21)00492-X
S1072	ZSTK474	ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.	J Cell Mol Med, 2021, 10.1111/jcmm.16889 Prostate, 2021, 10.1002/pros.24138 Exp Cell Res, 2021, 403(2):112615
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 Microbiol Spectr, 2022, e0188121 Cell Biol Toxicol, 2022, 10.1007/s10565-021-09670-5
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, 2021, 10.1007/s13577-021-00579-z Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
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 FEBS Lett, 2022, 10.1002/1873-3468.14273 Mol Biol Rep, 2022, 10.1007/s11033-021-07068-4
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 Metab, 2021, S1550-4131(21)00326-0 Cell Rep, 2021, 34(11):108870 Haematologica, 2021, 10.3324/haematol.2021.278743
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.	Cell Rep, 2021, 35(1):108940 Front Oncol, 2021, 11:620873 J Biol Methods, 2021, 8(1):e143
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.	J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R Front Med (Lausanne), 2021, 8:713312 Toxicology, 2021, 454:152747
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.	BMC Cancer, 2020, 20(1):4 Cell Rep, 2019, 27(3):820-834 Biochem Pharmacol, 2019, 169:113640
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.	Elife, 2021, 10e70715 Immun Inflamm Dis, 2021, 10.1002/iid3.458 Mol Cell, 2020, 79(1):191-198.e3
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.	Int J Mol Sci, 2021, 22(23)12673 Front Pharmacol, 2021, 12:743837 Toxicology, 2021, 454:152747
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 Cell Int, 2021, 21(1):24 Cancer Cell, 2020, S1535-6108(20)30427-X Proc Natl Acad Sci U S A, 2020, 117(39):24427-24433
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 (CAL-101, GS-1101)	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.	Nat Commun, 2022, 13(1):182 Cell Biol Toxicol, 2022, 10.1007/s10565-021-09670-5 Mol Cell, 2021, 81(4):708-723.e5
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, 2021, S1535-6108(21)00284-1 Adv Sci (Weinh), 2021, e2103360 Mol Cell, 2021, S1097-2765(21)00232-X
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 Nucleic Acids Res, 2021, gkab538 Redox Biol, 2021, 44:102010
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.	Cell, 2021, 184(25):6119-6137.e26 Mol Oncol, 2021, 10.1002/1878-0261.13031 Cancer Cell Int, 2021, 21(1):108
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 Biol Rep, 2022, 10.1007/s11033-021-07068-4 Proc Natl Acad Sci U S A, 2021, 118(19)e2017645118 J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R
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 Immunity, 2021, S1074-7613(21)00069-8 Cell Res, 2021, 10.1038/s41422-021-00528-3
S2658	Omipalisib (GSK2126458)	Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with K_i 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 Metab, 2021, S1550-4131(21)00326-0 Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-1943 Cancer Res, 2021, canres.3199.2020
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 K_i 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.	Adv Sci (Weinh), 2021, e2103360 Cancers (Basel), 2021, 13(9)2139 Commun Biol, 2021, 4(1):1333
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.	Cells, 2021, 10(5)1261 Mol Cells, 2021, 44(1):50-62 Cancer Lett, 2019, 443:135-144
S2743	PF-04691502	PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with K_i 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.	Cells, 2021, 10(5)1261 J Cell Physiol, 2021, 10.1002/jcp.30657 Front Pharmacol, 2021, 12:749242
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.	Cancer Biol Ther, 2017, 18(10):816-826 Oncotarget, 2016, 7(34):55690-55703 Oncotarget, 2016, 7(48):79842-79853
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.	Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119 Adv Sci (Weinh), 2021, e2004303 J Extracell Vesicles, 2021, 10(8):e12091
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.	Blood Cancer J, 2021, 11(6):111 Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0 Exp Hematol Oncol, 2021, 10(1):19
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.	Cell Death Dis, 2022, 13(1):46 FASEB J, 2022, 36(2):e22148 Bone, 2022, 154:116262
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.	Genome Med, 2021, 13(1):146 Autophagy, 2021, 10.1080/15548627.2021.1990670 Exp Neurol, 2021, S0014-4886(21)00200-4
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.	Sci Adv, 2022, 8(2):eabh3375 Oncoimmunology, 2022, 11(1):2021619 Cancer Cell, 2021, S1535-6108(21)00284-1
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 Nucleic Acids Res, 2021, gkab584 Cell Rep, 2021, 37(3):109854
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.
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.
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.
S3355	3-Hydroxyanthranilic acid	3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
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^New	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.
S6516	GNE-477	GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and K_iapp 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.
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.	Autophagy, 2021, 1-19 J Cell Sci, 2019, 132(16)jcs231639 Sci Rep, 2019, 9(1):5309
S7028	Duvelisib (IPI-145)	Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with K_i 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.	Eur J Cancer, 2021, 157:450-463 Eur J Cancer, 2021, 157:450-463 Front Oncol, 2021, 11:733848
S7103	Taselisib (GDC 0032)	Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with K_i of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.	Nat Cell Biol, 2021, 23(1):75-86 Cancer Res, 2021, canres.3232.2020 Mol Cells, 2021, 44(1):50-62
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.	Cell Death Dis, 2021, 12(8):713 Genome Med, 2020, 18;12(1):17 Cell Oncol (Dordr), 2020, 8
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.	Front Immunol, 2021, 12:761326 Genome Med, 2020, 18;12(1):17 Mol Cancer Ther, 2020, molcanther.1160.2019
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, 2021, 1-18 Autophagy, 2021, 1-16 Cell Death Dis, 2021, 12(11):1028
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 Sci Adv, 2021, 7(40):eabj2485 Oxid Med Cell Longev, 2021, 2021:7654143
S7694	AZD8186	AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.	Mol Cancer Ther, 2022, 21(1):170-183 Nat Commun, 2021, 12(1):5053 Front Oncol, 2021, 11:683629
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 (GSK2269557)	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, 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.	Nat Genet, 2021, 53(4):435-444 Cell Rep, 2021, 35(1):108940 Sci Rep, 2021, 11(1):9011
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.	Cancer Res, 2021, canres.0955.2021 Front Oncol, 2020, 10;10:331 Small GTPases, 2020, 10.1080/21541248
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.	Biomedicines, 2021, 9(5)579 Cell, 2019, 176(3):505-519 Cancer Res, 2019, 79(1):99-113
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.	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.	Sci Signal, 2021, 14(714):eabj0057 Exp Mol Med, 2020, 22 Front Immunol, 2020, 11:606893
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.	Cell Rep, 2021, 37(4):109899 Cell, 2020, S0092-8674(20)31394-5 bioRxiv, 2020, 10.1101/2020.11.18.388306
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).
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.	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^New	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.
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].
S8696	2-D08	2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.	Nat Commun, 2021, 12(1):4794 Cancers (Basel), 2021, 13(14)3475 Cancer Sci, 2021, 112(10):4075-4086
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.	Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140 Cancer Cell Int, 2021, 21(1):24 Oncol Rep, 2020, 43(3):773-782
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^New	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	Zandelisib (ME-401)	Zandelisib (ME-401, PWT-143, P110δ-IN-1, PW 143, ACC-524) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
S8948^New	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
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
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.	Oncol Rep, 2022, 47(1)18 Clin Sci (Lond), 2021, CS20210571 Front Cell Neurosci, 2021, 15:768364
S4572^New	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, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
E0020^New	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^New	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.
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.
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 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.	Sci Rep, 2022, 12(1):241 Curr Res Pharmacol Drug Discov, 2022, 3:100076 Nat Commun, 2021, 12(1):7268
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.	Adv Healthc Mater, 2021, e2101944 Cell Chem Biol, 2021, S2451-9456(21)00254-3 Neurobiol Dis, 2021, 156:105407
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.	Nat Commun, 2022, 13(1):245 Cancer Cell, 2021, S1535-6108(21)00383-4 Cancer Cell, 2021, S1535-6108(21)00492-X
S1072	ZSTK474	ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.	J Cell Mol Med, 2021, 10.1111/jcmm.16889 Prostate, 2021, 10.1002/pros.24138 Exp Cell Res, 2021, 403(2):112615
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 Microbiol Spectr, 2022, e0188121 Cell Biol Toxicol, 2022, 10.1007/s10565-021-09670-5
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, 2021, 10.1007/s13577-021-00579-z Hum Cell, 2021, 10.1007/s13577-021-00639-4 Hum Cell, 2021, 34(6):1911-1918
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 FEBS Lett, 2022, 10.1002/1873-3468.14273 Mol Biol Rep, 2022, 10.1007/s11033-021-07068-4
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 Metab, 2021, S1550-4131(21)00326-0 Cell Rep, 2021, 34(11):108870 Haematologica, 2021, 10.3324/haematol.2021.278743
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.	Cell Rep, 2021, 35(1):108940 Front Oncol, 2021, 11:620873 J Biol Methods, 2021, 8(1):e143
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.	J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R Front Med (Lausanne), 2021, 8:713312 Toxicology, 2021, 454:152747
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.	BMC Cancer, 2020, 20(1):4 Cell Rep, 2019, 27(3):820-834 Biochem Pharmacol, 2019, 169:113640
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.	Elife, 2021, 10e70715 Immun Inflamm Dis, 2021, 10.1002/iid3.458 Mol Cell, 2020, 79(1):191-198.e3
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.	Int J Mol Sci, 2021, 22(23)12673 Front Pharmacol, 2021, 12:743837 Toxicology, 2021, 454:152747
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 Cell Int, 2021, 21(1):24 Cancer Cell, 2020, S1535-6108(20)30427-X Proc Natl Acad Sci U S A, 2020, 117(39):24427-24433
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 (CAL-101, GS-1101)	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.	Nat Commun, 2022, 13(1):182 Cell Biol Toxicol, 2022, 10.1007/s10565-021-09670-5 Mol Cell, 2021, 81(4):708-723.e5
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, 2021, S1535-6108(21)00284-1 Adv Sci (Weinh), 2021, e2103360 Mol Cell, 2021, S1097-2765(21)00232-X
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 Nucleic Acids Res, 2021, gkab538 Redox Biol, 2021, 44:102010
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.	Cell, 2021, 184(25):6119-6137.e26 Mol Oncol, 2021, 10.1002/1878-0261.13031 Cancer Cell Int, 2021, 21(1):108
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 Biol Rep, 2022, 10.1007/s11033-021-07068-4 Proc Natl Acad Sci U S A, 2021, 118(19)e2017645118 J Leukoc Biol, 2021, 10.1002/JLB.2A0220-127R
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 Immunity, 2021, S1074-7613(21)00069-8 Cell Res, 2021, 10.1038/s41422-021-00528-3
S2658	Omipalisib (GSK2126458)	Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with K_i 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 Metab, 2021, S1550-4131(21)00326-0 Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-21-1943 Cancer Res, 2021, canres.3199.2020
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 K_i 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.	Adv Sci (Weinh), 2021, e2103360 Cancers (Basel), 2021, 13(9)2139 Commun Biol, 2021, 4(1):1333
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.	Cells, 2021, 10(5)1261 Mol Cells, 2021, 44(1):50-62 Cancer Lett, 2019, 443:135-144
S2743	PF-04691502	PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with K_i 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.	Cells, 2021, 10(5)1261 J Cell Physiol, 2021, 10.1002/jcp.30657 Front Pharmacol, 2021, 12:749242
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.	Cancer Biol Ther, 2017, 18(10):816-826 Oncotarget, 2016, 7(34):55690-55703 Oncotarget, 2016, 7(48):79842-79853
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.	Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119 Adv Sci (Weinh), 2021, e2004303 J Extracell Vesicles, 2021, 10(8):e12091
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.	Blood Cancer J, 2021, 11(6):111 Cancer Chemother Pharmacol, 2021, 10.1007/s00280-020-04210-0 Exp Hematol Oncol, 2021, 10(1):19
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.	Cell Death Dis, 2022, 13(1):46 FASEB J, 2022, 36(2):e22148 Bone, 2022, 154:116262
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.	Genome Med, 2021, 13(1):146 Autophagy, 2021, 10.1080/15548627.2021.1990670 Exp Neurol, 2021, S0014-4886(21)00200-4
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.	Sci Adv, 2022, 8(2):eabh3375 Oncoimmunology, 2022, 11(1):2021619 Cancer Cell, 2021, S1535-6108(21)00284-1
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 Nucleic Acids Res, 2021, gkab584 Cell Rep, 2021, 37(3):109854
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.
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.
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.
S3355	3-Hydroxyanthranilic acid	3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
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^New	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.
S6516	GNE-477	GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and K_iapp 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.
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.	Autophagy, 2021, 1-19 J Cell Sci, 2019, 132(16)jcs231639 Sci Rep, 2019, 9(1):5309
S7028	Duvelisib (IPI-145)	Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with K_i 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.	Eur J Cancer, 2021, 157:450-463 Eur J Cancer, 2021, 157:450-463 Front Oncol, 2021, 11:733848
S7103	Taselisib (GDC 0032)	Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with K_i of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.	Nat Cell Biol, 2021, 23(1):75-86 Cancer Res, 2021, canres.3232.2020 Mol Cells, 2021, 44(1):50-62
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.	Cell Death Dis, 2021, 12(8):713 Genome Med, 2020, 18;12(1):17 Cell Oncol (Dordr), 2020, 8
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.	Front Immunol, 2021, 12:761326 Genome Med, 2020, 18;12(1):17 Mol Cancer Ther, 2020, molcanther.1160.2019
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, 2021, 1-18 Autophagy, 2021, 1-16 Cell Death Dis, 2021, 12(11):1028
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 Sci Adv, 2021, 7(40):eabj2485 Oxid Med Cell Longev, 2021, 2021:7654143
S7694	AZD8186	AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.	Mol Cancer Ther, 2022, 21(1):170-183 Nat Commun, 2021, 12(1):5053 Front Oncol, 2021, 11:683629
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 (GSK2269557)	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, 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.	Nat Genet, 2021, 53(4):435-444 Cell Rep, 2021, 35(1):108940 Sci Rep, 2021, 11(1):9011
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.	Cancer Res, 2021, canres.0955.2021 Front Oncol, 2020, 10;10:331 Small GTPases, 2020, 10.1080/21541248
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.	Biomedicines, 2021, 9(5)579 Cell, 2019, 176(3):505-519 Cancer Res, 2019, 79(1):99-113
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.	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.	Sci Signal, 2021, 14(714):eabj0057 Exp Mol Med, 2020, 22 Front Immunol, 2020, 11:606893
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.	Cell Rep, 2021, 37(4):109899 Cell, 2020, S0092-8674(20)31394-5 bioRxiv, 2020, 10.1101/2020.11.18.388306
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).
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.	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^New	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.
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].
S8696	2-D08	2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.	Nat Commun, 2021, 12(1):4794 Cancers (Basel), 2021, 13(14)3475 Cancer Sci, 2021, 112(10):4075-4086
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.	Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140 Cancer Cell Int, 2021, 21(1):24 Oncol Rep, 2020, 43(3):773-782
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^New	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	Zandelisib (ME-401)	Zandelisib (ME-401, PWT-143, P110δ-IN-1, PW 143, ACC-524) is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay.
S8948^New	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
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
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.	Oncol Rep, 2022, 47(1)18 Clin Sci (Lond), 2021, CS20210571 Front Cell Neurosci, 2021, 15:768364
S4572^New	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, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
E0020^New	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^New	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.
S5978^New	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.
S8668^New	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.
S8779^New	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.
S8948^New	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.
S4572^New	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.