PI3K

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1009	Dactolisib (BEZ235, NVP-BEZ235)	<1 mg/mL	0.01 mg/mL	<1 mg/mL
S1065	Pictilisib (GDC-0941)	<1 mg/mL	44 mg/mL	<1 mg/mL
S1105	LY294002	<1 mg/mL	36 mg/mL	21 mg/mL
S2226	Idelalisib (CAL-101, GS-1101)	<1 mg/mL	83 mg/mL	23 mg/mL
S2247	Buparlisib (BKM120, NVP-BKM120)	<1 mg/mL	82 mg/mL	2 mg/mL
S8560	Seletalisib (UCB-5857)	<1 mg/mL	97 mg/mL	97 mg/mL
S8696	2-D08	<1 mg/mL	54 mg/mL	<1 mg/mL
S8672	Tenalisib (RP6530)	<1 mg/mL	75 mg/mL	75 mg/mL
S7335	IPI-3063	<1 mg/mL	91 mg/mL	12 mg/mL
S1038	PI-103	<1 mg/mL	24 mg/mL	<1 mg/mL
S2638	NU7441 (KU-57788)	<1 mg/mL	4 mg/mL	<1 mg/mL
S1169	TGX-221	<1 mg/mL	12 mg/mL	<1 mg/mL
S1268	IC-87114	<1 mg/mL	0.66 mg/mL	<1 mg/mL
S2758	Wortmannin	<1 mg/mL	85 mg/mL	<1 mg/mL
S1118	XL147 analogue	<1 mg/mL	3 mg/mL	<1 mg/mL
S1072	ZSTK474	<1 mg/mL	21 mg/mL	<1 mg/mL
S2814	Alpelisib (BYL719)	<1 mg/mL	88 mg/mL	2 mg/mL
S1410	AS-605240	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S1205	PIK-75 HCl	<1 mg/mL	4 mg/mL	<1 mg/mL
S2767	3-Methyladenine (3-MA)	10 mg/mL	3 mg/mL	4 mg/mL
S2636	A66	<1 mg/mL	79 mg/mL	1 mg/mL
S1523	Voxtalisib (SAR245409, XL765) Analogue	<1 mg/mL	12 mg/mL	<1 mg/mL
S1489	PIK-93	<1 mg/mL	78 mg/mL	<1 mg/mL
S2658	Omipalisib (GSK2126458, GSK458)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1187	PIK-90	<1 mg/mL	0.28 mg/mL	<1 mg/mL
S1462	AZD6482	<1 mg/mL	82 mg/mL	10 mg/mL
S2743	PF-04691502	<1 mg/mL	14 mg/mL	<1 mg/mL
S2696	Apitolisib (GDC-0980, RG7422)	<1 mg/mL	20 mg/mL	<1 mg/mL
S1360	GSK1059615	<1 mg/mL	2 mg/mL	<1 mg/mL
S7028	Duvelisib (IPI-145, INK1197)	<1 mg/mL	83 mg/mL	<1 mg/mL
S2628	Gedatolisib (PF-05212384, PKI-587)	<1 mg/mL	2 mg/mL	<1 mg/mL
S1352	TG100-115	<1 mg/mL	9 mg/mL	<1 mg/mL
S2671	AS-252424	<1 mg/mL	61 mg/mL	<1 mg/mL
S2749	BGT226 (NVP-BGT226)	<1 mg/mL	30 mg/mL	<1 mg/mL
S2759	CUDC-907	<1 mg/mL	102 mg/mL	<1 mg/mL
S2227	PIK-294	<1 mg/mL	98 mg/mL	<1 mg/mL
S2681	AS-604850	<1 mg/mL	57 mg/mL	5 mg/mL
S8002	GSK2636771	<1 mg/mL	28 mg/mL	<1 mg/mL
S2802	Copanlisib (BAY 80-6946)	0.002 mg/mL	0.002 mg/mL	0.01 mg/mL
S1219	YM201636	<1 mg/mL	35 mg/mL	<1 mg/mL
S2699	CH5132799	<1 mg/mL	12 mg/mL	<1 mg/mL
S2682	CAY10505	<1 mg/mL	58 mg/mL	<1 mg/mL
S2207	PIK-293	<1 mg/mL	80 mg/mL	<1 mg/mL
S2739	PKI-402	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S2870	TG100713	<1 mg/mL	2 mg/mL	<1 mg/mL
S7016	VS-5584 (SB2343)	<1 mg/mL	71 mg/mL	3 mg/mL
S7103	Taselisib (GDC 0032)	<1 mg/mL	70 mg/mL	<1 mg/mL
S7018	CZC24832	<1 mg/mL	5 mg/mL	<1 mg/mL
S7813	AMG319	<1 mg/mL	77 mg/mL	77 mg/mL
S7938	GSK2292767	<1 mg/mL	100 mg/mL	<1 mg/mL
S8163	GDC-0084	<1 mg/mL	8 mg/mL	<1 mg/mL
S8157	GDC-0326	<1 mg/mL	76 mg/mL	19 mg/mL
S7356	HS-173	<1 mg/mL	84 mg/mL	<1 mg/mL
S8589	SF2523	<1 mg/mL	29 mg/mL	7 mg/mL
S8581	Serabelisib (INK-1117,MLN-1117,TAK-117)	<1 mg/mL	16 mg/mL	<1 mg/mL
S8330	IPI-549	<1 mg/mL	100 mg/mL	8 mg/mL
S2391	Quercetin	<1 mg/mL	61 mg/mL	10 mg/mL
S8456	VPS34 inhibitor 1 (Compound 19, PIK-III analogue)	<1 mg/mL	78 mg/mL	<1 mg/mL
S7646	Voxtalisib (XL765, SAR245409)	<1 mg/mL	54 mg/mL	<1 mg/mL
S8596	Autophinib	<1 mg/mL	69 mg/mL	<1 mg/mL
S7798	GNE-317	<1 mg/mL	47 mg/mL	<1 mg/mL
S8194	umbralisib (TGR-1202)	<1 mg/mL	100 mg/mL	7 mg/mL
S7937	Nemiralisib (GSK2269557)	<1 mg/mL	88 mg/mL	8 mg/mL
S8322	LY3023414	<1 mg/mL	47 mg/mL	61 mg/mL
S7980	VPS34-IN1	<1 mg/mL	85 mg/mL	85 mg/mL
S7682	SAR405	<1 mg/mL	88 mg/mL	88 mg/mL
S7683	PIK-III	<1 mg/mL	63 mg/mL	63 mg/mL
S7623	PI-3065	<1 mg/mL	50 mg/mL	<1 mg/mL
S7645	Pilaralisib (XL147)	<1 mg/mL	100 mg/mL	<1 mg/mL
S7966	AZD8835	<1 mg/mL	93 mg/mL	<1 mg/mL
S8132	Deguelin	<1 mg/mL	78 mg/mL	78 mg/mL
S7675	PF-4989216	<1 mg/mL	76 mg/mL	7 mg/mL
S7694	AZD8186	<1 mg/mL	91 mg/mL	35 mg/mL
S7865	740 Y-P (PDGFR 740Y-P)	1 mg/mL	-1 mg/mL	-1 mg/mL

Isoform-specific Inhibitors

PI3K Inhibitors (74)
New PI3K Products

Catalog No.	Information	Product Use Citations	Product Validations
S1009	Dactolisib (BEZ235, NVP-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.	Nature, 2018, 560(7718):372-376 Nature, 2017, 543(7647):728-732 Nature, 2017, 728-732	Level of phospho-proteins in RTK and PI3K–Akt–mTOR pathways in treated tumours, detected with western blot.
S1065	Pictilisib (GDC-0941) Pictilisib (GDC-0941) 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). Phase 2.	Nature, 2014, 508(7494):118-22 Cancer Discov, 2011, 1(7):608-25 Cell Stem Cell, 2012, 10(2):210-7	Clonogenic assays of TNBC cell lines grown continuously in increasing concentrations of palbociclib, divided by gene expression subtypes: LAR, luminal androgen receptor; MSL, mesenchymal stem-like; MES, mesenchymal and basal-like. All cell lines are RB1 wild-type except RB1 mutant BT549.
S1105	LY294002 LY294002 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.	Nature, 2015, 10.1038/nature14412 Am J Respir Crit Care Med, 2015, 10.1164/rccm.201501-0188OC Blood, 2014, 123(2):239-48	Type I IFNs induce ISG expression in a serine phosphorylation-independent manner. Cells were treated with kinase inhibitors (SB203580, rottlerin, Ly294002, PD98059, and SP600125) before stimulation with IFN-a and IFN-b for 6 hours. Cell lysates were used in western blotting and probed for serine phosphorylation.The relative amounts of pSTAT1 S727 in (up-graph) were quantied and normalized to an untreated control (below-graph).
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.	Nature, 2017, 552(7683):121-125 Nature, 2016, 539(7629):437-442 Nature, 2015, 517(7535):460-5	Invasive migration of RA FLS was analyzed through growth factor–reduced Matrigel-coated transwell inserts in the presence or absence of 1 µM INK007, 5 µM CAL-101, or 0.3 µM IPI-145, or 0.3 µM GDC-0941 inhibitors or DMSO. Cells were allowed to invade through Matrigel toward PDGF-BB (25 ng/ml) containing media for 24 h and were fixed and stained with Hemacolor staining kit.
S2247	Buparlisib (BKM120, NVP-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. Phase 2.	Nat Med, 2015, 10.1038/nm.3855 Cell, 2017, 161(4):803-16 Cancer Discov, 2013, 4(2):232-45	NLGN3 mRNA expression in SU-pcGBM2 cells after 12 hr exposure to vehicle, 50 nM NLGN3, 100 nM BKM120, or 50 nM NLGN3 + 100 nM BKM120.
S8560^New	Seletalisib (UCB-5857) Seletalisib 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).
S8696^New	2-D08 2-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, 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.
S8672^New	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.
S7335^New	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.
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.	Cell, 2013, 153(4):840-54 Leukemia, 2013, 27(3):650-60 Leukemia, 2012, 26(5):927-33	(D) IGROV parental, shControl (two independent clones) and ShPKCiota (two independent clones) were treated with 5 μM GDC-0941 and 1.5 μM PI-103 for 24 hours and subjected to western blot analysis with the indicated antibodies. Each experiment was performed in triplicate.
S2638	NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM in cell-free assays. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.	Nucleic Acids Res, 2017, 45(1):244-254 Nucleic Acids Res, 2014, 42(12):7776-92 Nucleic Acids Res, 2014, 42(9):5616-32	Cells were treated with cisplatin under the following conditions: pretreatment with Nu7026 (Nu7026, 26) or Nu7441 (Nu7441, 41). Before DNA damage, wortmannin was applied at 100 nM for 30 min, Nu7026 at 10 uM for 1 h, Nu7441 at 1 uM for 1 h. Accompanying quantifications of the adjusted nucleolar EU fluorescence are shown. Each condition was normalized to cells treated with DMSO or indicated inhibitors without DNA damaging treatment. Two-way ANOVA was followed by Holm-Sidak's test for the comparison of cells with and without inhibitors. , , ** represent P ≤ 0.05, 0.01, 0.001, respectively.
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.	Cancer Cell, 2015, 27(1):97-108 Blood, 2014, 123(2):239-49 Cell Death Differ, 2013, 21(3):491-502	A p110β-selective antagonist rescues increased protein synthesis in synaptic fractions from Fmr1 KO mice and in LCLs from a patient with FXS. (A–C) Treatment of synaptoneurosomes with TGX-221 (1 μmol/L, 30 min) reduces p110β-specific PI3K activity and phosphorylation of the downstream target AKT in both WT and Fmr1 KO SNS, shown by a radioactive PI3K assay and phosphoAkt- specific western blot-ting (A). (B) Quantification of PI3K activity using a competitive ELISA showed a significant reduction in PI3K activity in both genotypes after treatment [ n = 4, 2-way ANOVA, P (genotype) = 0.0086, P (treatment) = 0.0087, P (interaction) = 0.7154]. (C) Densitometric quantification of phosphoAkt-specific western blots showed a significant effect of treatment (C, n = 4, 2-way ANOVA, *P (treatment) = 0.0005, P (genotype) =0.372, P (interaction) = 0.4894).
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.	Cancer Discov, 2012, 2(5):425-33 Cancer Cell, 2015, 27(1):97-108 Cancer Immunol Res, 2014, 2(11):1080-9
S2758	Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.	Nature, 2015, 10.1038/nature14412 Science, 2016, 353(6302):929-32 Cancer Res, 2014, 74(10):2846-56	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
S1118	XL147 analogue XL147 analogue 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.	Autophagy, 2012, 8(6):903-14 Cancer Res, 2014, 74(18):5184-94 Oncogene, 2015, 10.1038/onc.2015.143	Breast cancer cells were pretreated with 100ng/ml EGF for 20 min and then treated with the indicated concentrations of XL147 for 24 hours.
S1072	ZSTK474 ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2.	NAT MATER, 2017, 10.1038/NMAT5024 J Cell Sci, 2014, 127(Pt 4):788-800 J Cell Mol Med, 2015, 19(9):2244-52	j,k, Gene expression ofMYOCD (j) and ACTA2 ( SMA, k) after applying inhibitors of key components involved in the DDR2 downstream signalling pathway to HSCs cultured within 3D collagen matrix subjected to stretching (ST) (n=3, one-way ANOVA, P=0.0036, P<0.0001). l,m, Expression of SMA was significantly reduced after treatment with related inhibitors in early-stage FμNs. (n=4, one-way ANOVA, P=0.001, ***P<0.0001). PI3K-i: ZSTK474
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.	Blood, 2015, 10.1182/blood-2014-11-610329 J Thorac Oncol, 2015, 10(12):1736-44 Oncogene, 2016, 10.1038/onc.2016.216	AN3CA (B), JHUEM2 (D), and MFE296 (H) cells were treated with the indicated doses of BGJ398 and BYL719 alone or in combination for 96 hours, and an SRB assay was subsequently performed.
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.	Blood, 2015, 10.1182/blood-2014-11-610329 J Pharmacol Exp Ther, 2013, 347(3):669-80 Exp Gerontol, 2014, 52:55-69	After starved in serum-free medium for 24 h, Breast cancer cells incubated with the indicated concentrations of AS-605240 for 3 h,followed by 15-minute stimolation of 100ng/ml EGF
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 Death Differ, 2013, 21(3):491-502 J Exp Clin Cancer Res, 2016, 35(1):78 Stem Cells, 2015, 10.1002/stem.1986	A549 cells were treated with DMSO or PIK-75 (200 nM) for 1 h and subsequently stimulated with izTRAIL for 24 h. Long-term survival was visualized after 7 days by crystal violet staining. One of two independent experiments is shown.
S2767	3-Methyladenine (3-MA) 3-Methyladenine (3-MA) 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.	Cell Death Dis, 2016, 7(6):e2247 Cell Physiol Biochem, 2016, 38(6):2401-13 Am J Cancer Res, 2015, 5(1):125-139	MDC-labeled vacuoles were induced by AZD2014 and inhibited by autophagy inhibitor (3-MA). SMMC-7721 cells were treated with AZD2014 or rapamycin at concentrations of 100 and 600 nM, respectively, for 48 hours in the presence or absence of 3-MA, and then stained with MDC. Cells were immediately observed under a confocal microscope. Cells in the control group were treated with DMSO. bars, 20 μm.
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.	Nature, 2015, 517(7535):460-5 Genes Dev, 2012, 26(14):1573-86 Cell Death Differ, 2013, 21(3):491-502	(C) Western blot analyses of pAkt in MMTV-MT tumor derived cells treated with various PI3K inhibitors (in micromolar) as indicated following growth factor starvation. (D) Western blot analyses of pAkt in MMTV-NeuT tumor-derived cells treated with various PI3K inhibitors (in micromolar) as indicated. () P < 0.01; (*) P < 0.001 (Student’s t-test).
S1523	Voxtalisib (SAR245409, 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 Rep, 2015, 11(3):446-59 Mol Cancer Res, 2014, 12(5):703-13 Endocrinology, 2013, 154(3):1247-59	The TMZ/XL765 combination decreases serum GH and PRL of mice bearing GH3 xenografts. A and B, After treatment with DMSO, TMZ, XL765, or the XL765/TMZ combination, the blood of the nude mice xenograft with GH3 tumor was collected and serum rat-GH and rat-PRL were measured by IRMA (TMZ/XL765 combination vs TMZ or XL765 alone: ***P <.001).
S1489	PIK-93 PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM.	Mol Cell Endocrinol, 2013, 372(1-2):86-95 PLoS One, 2015, 10(3):e0122753	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of PIK-93 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S2658	Omipalisib (GSK2126458, GSK458) 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. Phase 1.	Proc Natl Acad Sci USA, 2013, 110(10):4015-20 Neuro Oncol, 2016, 18(4):528-37 Mol Cancer Ther, 2015, 14(2):429-39
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.	J Cell Biol, 2012, 198(2):185-94 Exp Mol Med, 2015, 47:e143 J Cell Mol Med, 2013, 17(5):648-56	3D cultures expressing control (pQCXIP GFP) or K-Ras V12 (pQCXIP GFP K-Ras V12) were continuously treated with 5, 10, or 20 uM of the MEK inhibitor U0126 or 2.0 uM of the PI3K inhibitor PIK-90. At day 10, these structures were fixed and stained for aPKC and DNA. Representative images are shown. Bar, 50 um.
S1462	AZD6482 AZD6482 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.	Blood, 2014, 125(5):881-8 Breast Cancer Res, 2016, 10.1186/s13058-016-0697-1 Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268	Collagen-embedded melanoma spheroids were treated for 72 h with SGI-1776 [5 μM] or AZD6482 [10 μM] as single agents or in combination before staining for live (green) and dead (red) cells. Experiments were conducted in triplicate and representative images are shown. Scale bar represents 150 microns.
S2743	PF-04691502 PF-04691502 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. Phase 2.	Blood, 2015, 10.1182/blood-2014-11-610329 Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-16-1971 Cell Rep, 2015, 11(3):446-59	BMDMs from WT animals were treated with different concentrations of PI3K inhibitors (500 nmol/L PF4691502, PI-103, BKM120 and 25 μmol/L SF1126) followed by hypoxia for 4 hours for Western blots. These macrophages were either used for lysate preparation (nuclear extracts for HIFα or WCE for pAKT and AKT) and Western blot analysis.
S2696	Apitolisib (GDC-0980, RG7422) Apitolisib (GDC-0980, RG7422) 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. Phase 2.	Cancer Discov, 2014, 4(5):554-63 Breast Cancer Res, 2014, 16(4):406 Mol Cancer Ther, 2015, 14(8):1928-38	Immunoblots from AR + TNBC cell lines treated with either CDX (25 uM), GDC-0941 (300 nM) or GDC0980 (100 nM) as single agents or CDX in combination with either GDC-0941 or GDC-0980 for 48 h analyzed for AR, p-AKT, AKT, p-S6, S6 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH) protein.
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.	Nature, 2012, 486(7404):532-6 Nat Chem Biol, 2013, 9(11):708-14 Exp Mol Med, 2015, 47:e143	The PI3K/AKT pathway significantly contributes to the ligand-driven HER2 signaling activities detected by CELx HSF tests. a and b SKBr3 cells were seeded in sensor plates and then treated with a serial titration of the PI3K/AKT pathway inhibitor GSK1059615 (0 nM to 810 nM) two hours prior to maximal stimulation with NRG1b (800 pM) (a) or EGF (600 pM) (b). CELx curves are displayed using Delta CI values to demonstrate the relative signals to the time point (arrow) when the stimulus (EGF or NRG1b) was added. Dose–response curves of GSK1059615 inhibition on NRG1b and EGF-driven HER2 signals are shown in the insets
S7028	Duvelisib (IPI-145, INK1197) 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.	Blood Cancer J, 2017, 7(3):e539 Int J Cancer, 2015, 10.1002/ijc.29579 PLoS One, 2016, 11(12):e0169230	MM1s were incubated with increasing doses of duvelisib for 4 h after which protein was extracted. Samples were then analysed for phospho-AKT and phospho-MAPK response using Western blotting. Blots were re-probed for total AKT and MAPK to confirm sample loading.
S2628	Gedatolisib (PF-05212384, 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 Rep, 2015, 11(3):446-59 Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268 Mol Cancer Ther, 2015, 14(2):429-39	PI3K inhibitors promote apoptosis in checkpoint-defective cell lines. Two checkpoint-functional (A2058, D28) and three defective (HT144, D20, SKMel13) melanoma cell lines growth as tumour spheres as in Figure 4B were either untreated or treated with 5 uM PF-05212384 for 72 h, harvested and immunoblotted for pAkt Ser473.
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.	Exp Mol Med, 2015, 47:e143 Biochim Biophys Acta, 2017, 1861(4):947-957 Biochim Biophys Acta, 2017, 1861(4):947-957	(E) Phosphorylation of CREB affected by different concentrations of TG100-115 determined by using immunoblotting
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.	Blood, 2014, 123(2):239-51 Cell Death Differ, 2014, 21(3):491-502 Pigment Cell Melanoma Res, 2014, 10.1111/pcmr.12268	Effects of AS252424 on KL-induced cPLA 2 phosphorylation in BMMCs. BMMCs were pre-incubated with AS252424 for 1 h followed by stimulation with KL for 15 min. The phosphorylation of cPLA 2 was evaluated via immunoblot analysis. Results are representative of three independent experiments.P<0.05, P<0.01, **P<0.001 and ### P<0.001, compared with BMMCs with KL induction but without pretreatment by AS252424.
S2749	BGT226 (NVP-BGT226) BGT226 (NVP-BGT226) 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 Lett, 2014, 348(1-2):38-49 Mol Cancer Ther, 2015, 14(8):1928-38 PLoS One, 2014, 9(3):e90746	IGROV1-R10 cells were treated with BGT266(250nM) for 8 h.The effect of BGT226 on PI3K/Akt/mTOR pathway activation (A) and on expression of Mcl-1 and Bim (B).
S2759	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. Phase 1.	Stem Cells Dev, 2017, 26(5):353-362 Am J Transl Res, 2014, 6(5):471-493 Saudi J Gastroenterol, 2017, 23(1):34-38	Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
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.	Mol Cell Biol, 2012, 32(12):2268-78	After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PIK-294 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
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.	Nature, 2017, 542(7642):489-493 J Biol Chem, 2014, 289(46):32109-20	Numbers of AID on-target (Igh and Igk loci) and off-target hot spots from WT and AID−/− B cells. Data pooled from at least n = 3 biological replicates
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.	Blood, 2015, 10.1182/blood-2014-11-610329 Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-15-2764 Mol Pharmacol, 2016, 90(6):726-737	Cells were treated as indicated. Medium and drug were refreshed every 2 to 3 days, and protein lysates were analyzed as above.
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.	Nature, 2018, 560(7719):499-503 Oncol Rep, 2017, 37(5):3137-3145 Oncotarget, 2016, 7(15):19620-30	(A) Total cell lysates were immunoblotted with the indicated antibodies. β-actin served as the loading control.
S1219	YM201636 YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue).	FEBS Lett, 2016, 590(11):1576-85	Validation study for vacuolin-1 and YM201636. (A) HeLa cells were treated with 3 lM vacuolin-1 or YM201636 in the presence or absence of the lysosomal protease inhibitor E64d (10 μg/mL) and pepstatin A (10 μg/mL). After 24 h of treatment, cell lysates (10 μg) were separated by 10% polyacrylamide gel electrophoresis, and LC3 was detected via immunoblotting.
S2699	CH5132799 CH5132799 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	Effect of selected compounds on MLC phosphorylation induced by 2-AG. Washed platelets (1.0 x 10⁹ platelets/mL) were preincubated at 37 ℃ for 10 min with saline or 20 uM LY294002 (L), 10 uM CH5132799 (C), 10 uM TGX221 (T), 10 uM MK2206 (M), 20 uM Y27632 (Y), 1 uM PIK-75 (P), 1 U/mL apyrase (AP), 5 uM AS252424 (AS), 1 uM IC87114 (IC) and then stimulated for 30 s with 10 uM 2-AG. At the end of incubation suitable aliquots were immunoblotted with anti-p-MLC (thr18/ser19) as detailed in Methods. Blot is representative of four independent experiments.
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	(D) Box plots showing the results of primary MM cell treatment (n = 22; in co-culture with BMSCs) with PI3K inhibitors (10 umol/l each). BYL-719 exerted the strongest anti-myeloma effects of TGX-221, CAY10505 or CAL-101. The mean survival value is indicated by a horizontal bar and the end of the whiskers show the values of the most sensitive and most resistant sample, respectively. (E) Treatment of PBMCs (n = 5) for 5 d with PI3K isoform-specific inhibitors (10 umol/l each).
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.		After starved in serum-free medium for 24 h,A549 cells incubated with the indicated concentrations of PIK-293 for 3 h,followed by 20-minute stimolation of 100ng/ml EGF.
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.
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.	MedChemComm, 2013, 10.1039/c3md00301a	The compounds BAY80-6946 and TG100713, which are respectively an alpha/beta- and a pan-isoforms inhibitors, demonstrated a very good ability to block Jurkat E6.1 proliferation with an IC50 slightly higher than 1 mM.
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.	PLoS One, 2015, 10(7):e0132655 Platelets, 2017, 10.1080/09537104.2017.1306040	VS-5584 inhibits melanoma cell survival and proliferation-Established melanoma cell lines (A375, A-2058 and SK-MEL-3), patient-derived primary melanoma cells, B10BR melanocytes and primary human keratinocytes (“Kera”) were treated with applied concentration of VS-5585 (“VS”) or vehicle control (“C”, 0.1% of DMSO), cell survival was tested by MTT assay (A, E and F) and trypan blue exclusion assay (B, for A375 cells); Cell proliferation was analyzed by through [H3] Thymidine incorporation assay (C, for A375 cells) and clonogenicity assay (D, for A375 cells). Data were expressed as mean ± SD, experiments were repeated three times. *p<0.05 vs group “C”.
S7103	Taselisib (GDC 0032) Taselisib (GDC 0032) 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.
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.	Blood Cancer J, 2017, 7(3):e539 Cancer Cell Int, 2017, 10.1186/s12935-017-0396-8 Anticancer Res, 2015, 35(5):2699-708	(c) MM primary cells were treated with idelalisib (1 μm), CZC24832 (1 μm) and duvelisib (1 μm) for 72 h and then assessed for apoptosis by PI/Annexin V staining (n=4).
S7813	AMG319 AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
S7938	GSK2292767 GSK2292767 is a potent and selective PI3Kδ inhibitor.
S8163	GDC-0084 GDC-0084 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.
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.
S7356	HS-173 HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.	Cancer Cell Int, 2017, 10.1186/s12935-017-0396-8 Otorhinolaryngol Head Neck Surg, 2016, 1(2): 44-50	b, d Serum-deprived MG-63 (b) and U20S cells (d) were pre-treated with 1 nmol/L HS-173 (PI3Kα inhibitor), 10 nmol/L TGX-221 (PI3Kβ inhibitor), 10 nmol/L CZC24832 (PI3Kγ inhibitor) and 10 nmol/L CAL-101 (PI3Kδ inhibitor) for 1 h, then were incubated with 100 ng/mL Wnt5a and harvested at 30 min after the start of Wnt5a treatment. Data were presented as mean ± SD of 3 determinations. The relative RhoA activity was normalized to the average value of each inhibitor-untreated group
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.
S8581	Serabelisib (INK-1117,MLN-1117,TAK-117) Serabelisib (INK-1117,MLN-1117,TAK-117) 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.
S8330	IPI-549 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.
S2391	Quercetin Quercetin, 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. Phase 4.	Mol Nutr Food Res, 2017, 61(4)	After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Quercetin for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
S8456	VPS34 inhibitor 1 (Compound 19, PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.	Oncotarget, 2017, 8(24):38099-38112	Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2-/- MEFs treated with vehicle control (DMSO), CQ (5 uM), VPS34-IN1 (500 nM) or the combination for 72 hours (crystal violet staining). Two sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.
S7646	Voxtalisib (XL765, SAR245409) 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.	Int J Oncol, 2015, 47(3):1143-59	Cell viability measurements. The IMR-32, LA-N-1 and CHP‑134 cells were treated with mTOR/PI3K inhibitor SAR245409 alone or in combination with the 14G2a mAb (40 μg/ml) for 72 h. The cell viability was determined by measuring ATP content, and compared to respective controls treated with appropriate diluents (DMSO or water, set as 1). P-values for t-test were as follows: p<0.05, p<0.01, **p<0.001.
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.
S7798	GNE-317 GNE-317 is a potent, brain-penetrant PI3K inhibitor.
S8194	umbralisib (TGR-1202) TGR-1202, 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.
S7937	Nemiralisib (GSK2269557) Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
S8322	LY3023414 LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.		The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.
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.	Oncotarget, 2017, 8(24):38099-38112	C. Lysosomal and endosomal inhibition selectively targets Tsc2−/− MEFs. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), Vps34 inhibitor (SAR405; 1uM) or the combination for 72 hours (crystal violet staining). D. Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), VPS34-IN1 (500nM) or the combination for 72 hours (crystal violet staining). Two-sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.
S7682	SAR405 SAR405 is a low-molecular-mass kinase inhibitor of 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.
S7683	PIK-III PIK-III, 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.	Mol Biosyst, 2017, 13(10):1993-2005	LC3 and DAPI immunofluorescence staining were performed to detect autophagy in VSC4.1 cells treated with 25 mM HD alone, 25 mM HD + 5 μM PIK-III, 5 μM PIK-III and 0.1% DMSO alone (control group). Scale bar: 20 μm
S7623	PI-3065 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
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.	J Cell Mol Med, 2013, 17(11):1397-409	G, tumor growth response of HR6 tumors grown in athymic nude mice and treated with single and combination treatments. H, table of earliest detectable (P < 0.05) reduction in tumor size for control versus treated mice. ^, tumors that initially shrank and then grew; NS, not significant. I, OMI index initially decreases in HR6 organoids treated with paclitaxel, XL147, and combination therapies at 24 hours. J, OMI index of HR6 organoids treated for 72 hours. Red bars, significant reductions in OMI index; P< 0.05, for treated organoids versus control. Blue bars, significant increases in OMIindex;P< 0.05, for treated organoids versus control.
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).
S8132	Deguelin Deguelin, a natural product isolated from plants in the Mundulea sericea family, is an PI3K/AKT Inhibitor.
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.
S7694	AZD8186 AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.
S7865	740 Y-P (PDGFR 740Y-P) 740 Y-P is cell-permeable phosphopeptide activator of PI3K.

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