LY294002

Name: LY294002
Brand: MedChemExpress
SKU: HY-10108
Rating: 5.0 (835 reviews)

Cat. No.: HY-10108 Purity: 99.86%: FAQs
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LY294002 is a broad-spectrum inhibitor of PI3K with IC₅₀s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC₅₀ of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC₅₀ of 1.4?μM. LY294002 is an apoptosis activator.

For research use only. We do not sell to patients.

LY294002 Chemical Structure

CAS No. : 154447-36-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
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Based on 835 publication(s) in Google Scholar

Other Forms of LY294002:

LY294002 hydrochloride Get quote

780 Publications Citing Use of MCE LY294002

IHC

Proliferation Assay

: LY294002 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2023 May 22.; LY294002 (10 µM; 12 h) significantly increases the expression of C-caspase3 protein and decreases the expression of Bcl-2 protein in primary neuronal cells.

: LY294002 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2023 May 22.; LY294002 (10 µM; 12 h) significantly inhibits the proliferation of primary neuronal cells.

: LY294002 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 14.; Both of LY294002 (LY; 30 μM) and Wortmannin (Wort; 50 nM) can downregulate the expression of ACE2 in HPAEpiC cells.

: LY294002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453. [Abstract]; Western blot analysis of BAX and PARP (full length and cleaved PARP) expressions in treated LNCaP cells with the treatment of SAHA or RG7388.

: LY294002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453. [Abstract]; Apoptotic cell death in LNCaP cells shown by Fluorescence image obtained using the DEVD-amc. The results of cell death induced by SAHA and RG7388 treatment for 24 hrs are shown.

: LY294002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453. [Abstract]; Protein levels of p53, p21 and MDM2 are upregulated in LNCaP cells after treatment with 2.0 μM concentration of RG7388.

: LY294002 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Feb;234(2):1567-1577. [Abstract]; GRPR-1 gene silencing lowers the positive protein levels of GRPR in kidney tissues of mice detected by immunohistochemistry. The positive protein levels of GRPR by immunohistochemical staining (400×).

: LY294002 purchased from MedChemExpress. Usage Cited in: Biol Trace Elem Res. 2019 Aug;190(2):327-335. [Abstract]; Number of cells stained positive for ALP increase significantly after stimulation with orthosilicic acid for 72 h and decrease after stimulation with LY294002 for the last 48 h of this period.

: LY294002 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819. [Abstract]; Expression of E-cadherin and vimentin is regulated by COX‑2. MG‑63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (A) The expression of E-cadherin (green) in each group was determined using immunofluorescence. (B) Quantification of E‑cadherin expression.

: LY294002 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819. [Abstract]; Expression of E-cadherin and vimentin is regulated by COX‑2. MG‑63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (C) The expression of vimentin in each group. (D) Quantification of vimentin expression.

: LY294002 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819. [Abstract]; Expression of NF‑κB p65 protein is regulated by COX‑2. MG‑63 cells were infected with control or COX‑2‑overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (A)The expression of NF-κB p65 (green) in each group was determined by immunofluorescence. (B) Quantification of NF-κB p65 expression.

: LY294002 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jan;19(1):177-186. [Abstract]; Western analysis of p-AKT1 and AKT1 in the treatment of MCF7 alone, MCF7 co-cultured, anti-TGF-β1 and LY29400

: LY294002 purchased from MedChemExpress. Usage Cited in: J Neuropathol Exp Neurol. 2019 Feb 1;78(2):157-171. [Abstract]; Western analysis the protein expression of PI3K, p-mTOR, mTOR, p-AKT, AKT with or without the treatment of OGD, 450 μM GBP and 10 μM LY294002.

: LY294002 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 8;508(2):398-404. [Abstract]; TUNEL staining shows green fluorescence of apoptosis HK-2 cells with the treatment of HG+PPQ or HG+PPQ+LY294002.

: LY294002 purchased from MedChemExpress. Usage Cited in: Blood. 2018 Jul 12;132(2):210-222. [Abstract]; Phosphorylation of p-ERK1/2 and p-Akt in MKs pretreated with 0.5 μM NVP-ADW742, 10 μM U0126 or 20 μM LY294002 followed by rhIGF-1 treatment for 15 minutes.

: LY294002 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 13;37(1):189. [Abstract]; H1299 cells transfected with si-MKRN2 are treated or not treated with the PI3K inhibitor LY294002 analyzed by western blot for the expression of proteins involved in cell migration and invasion.

: LY294002 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122. [Abstract]; MHCC97H cells are treated with either LY294002 (2.5, 5,10, 20, 40 μM) or ZSTK474 (0.5, 1, 2.5, 5, 10 μM) for 24 h. DMSO is used as the control. Cell lysates are subjected to western blot analysis with the indicated antibodies.

: LY294002 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 5;37(1):46. [Abstract]; Treatment with LY294002 reverses Epithelial-mesenchymal transition (EMT) mediated by miR-10b overexpression. GAPDH is used as a loading control.

: LY294002 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269. [Abstract]; WB is used to detect the effect of EGF treatment for 4 h on the expression of YAP with the inhibitors of EGFR or its downsream members, including ZD1839, LY294002, Wortmannin, GSK2334470, BX-795, MK-2206, GSK1120212, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.

: LY294002 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2018 Nov;39(11):1787-1796. [Abstract]; Effects of LY294002 or AKT siRNA on the levels of total AKT, pAKT, phosphorylated PRAS40 and pMDM2 are examined by Western blot analysis in MCF-7 cells when HBXIP was overexpressed. Effects of MK-2206 or HBXIP siRNA on the levels of total AKT, pAKT, pPRAS40, and pMDM2 are examined by Western blot analysis in MCF-7-HBXIP cells.

: LY294002 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132. [Abstract]; Sertoli cells (SC) are pretreated with LY294002 at 20 μM for 1 h followed by a 24-h treatment with MC-LR. Expression levels of p-p65 and MMP-8 are detected by western blotting.

: LY294002 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1348-1356. [Abstract]; ECa109 and EC9706 cells are treated with 20 μM LY294002 for different time (0, 3, 6, 12, 24 h). Total proteins are extracted for the analysis of key proteins in PI3K/Akt/ mTOR signaling pathway by Western blot.

: LY294002 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1348-1356. [Abstract]; ECa109 and EC9706 cells are treated with various doses of LY294002 (0, 10, 20 μM) for 24 h. Total proteins are extracted for the analysis of key proteins in PI3K/Akt/ mTOR signaling pathway by Western blot.

: LY294002 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Jul;103:729-737. [Abstract]; Representative Western blots show the effect of PI3K inhibitor LY294002 treatment for 24 h on PI3K p110a, Akt phosphorylation (P-Akt) and mTOR phosphorylation (P-mTOR). Total Akt and GAPDH are also detected by Western blot.

: LY294002 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6). pii: E1556. [Abstract]; E-cadherin, N-cadherin, Snail, and MMP-2 expression in HCC cells is examined by Western blot analysis. GAPDH is used as a loading control.

: LY294002 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960. [Abstract]; Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in U87-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.

: LY294002 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960. [Abstract]; Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in T98G-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.

: LY294002 purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2018 Sep 1;57(9):1675-1684. [Abstract]; The hypoxia-aggravated phosphorylation of Akt and mTOR is inhibited by LY294002, a PI3K inhibitor (P<0.01), suggesting that hypoxia-induced Akt phosphorylation was through PI3K activation.

: LY294002 purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2018 Sep 1;57(9):1675-1684. [Abstract]; LY294002 and Rapamycin also down-regulates the HIF-1α expression under hypoxic condition (P<0.01) and inhibits hypoxia-induced expressions of CTGF (P<0.05) and collagen I (P<0.05 or P<0.01).

: LY294002 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365. [Abstract]; p-FOXO3a (Thr32), p-FOXO3a (Ser253), FOXO3a, p-Akt and Akt expression via western blot following treatment with PBS, ASV, TGF-b1, TGF-b1+ASV, TGF-b1+SB431542 or TGF-b1+LY294002.

: LY294002 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5311-5321. [Abstract]; The expression of PI3K, Akt, p-Akt, HO-1, LC3-II/LC3-I and Beclin-1 in LY294002 group after pharmorubicin treatment are examined by Western blot. The protein expression in LY294002 group is decreased.

: LY294002 purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Jan 11;12:137-148. [Abstract]; Effects of LY294002 on AKT and p-AKT expression of hPDLCs. (A) The increased expression of osteogenic marker proteins can be interdicted by PI3K pathway inhibitor LY294002 in hPDLCs. The expression level of ALP and Runx2 is tested by Western blot (B).

: LY294002 purchased from MedChemExpress. Usage Cited in: Neuropharmacology. 2018 Mar 15;131:190-199. [Abstract]; LY294002 blocks the regulatory effects of GLP-1RA on Akt, GSK-3β and GnT-III. The inhibitor LY294002 (10 μM) is added to PC12 cells 1 h before Aβ_25-35 and GLP-1RA treatment. The levels of p-Akt、total Akt、p-GSK3β、 total GSK-3β and GnT-III are detected by Western blot (n=3 per group).

: LY294002 purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2018 Feb;96(2):119-133. [Abstract]; The regulation of PHP14 on Akt phosphorylation is possibly via PI3Kγ in LX-2 cells. Cells are serum starvation 24 h, then treated TGF-β1 (10 ng/mL) 2 h, then added LY294002 (5 μM) or AS252424 (10 μM) as indicated; after another 2 h incubation, Western blot is performed to assess the protein expression of p-Akt.

: LY294002 purchased from MedChemExpress. Usage Cited in: Reprod Biol Endocrinol. 2018 May 31;16(1):55. [Abstract]; Western blot analysis of claudin 5, occludin and ZO-1 in TM4 cells, cells are treated with 100 nM Leptin or pre-treated with different inhibitors following a 100 nM Leptin treatment.

: LY294002 purchased from MedChemExpress. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832. [Abstract]; HSCs are pretreated with AICAR (500 μM), LY294002 (20 μM), PD98059 (10 μM), or Rapamycin (100 nM) for 2 h and then incubated with or without CoCl₂ (150 μM) for 12 h. Expression levels of HIF-1α and VEGF are measured by Western blot analysis;

: LY294002 purchased from MedChemExpress. Usage Cited in: Toxins (Basel). 2018 Sep 28;10(10). pii: E398. [Abstract]; Expression levels of p-AKT/AKT, p-mTOR/mTOR, and LC3II/LC3I after adding PI3K inhibitors (LY294002) in the experiments.

: LY294002 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2018 Oct 9;11:6693-6703. [Abstract]; LY294002, an Akt inhibitor, is applied to the inhibition on prolifera¬tion.

: LY294002 purchased from MedChemExpress. Usage Cited in: Cytokine. 2018 Jun;106:54-66. [Abstract]; Effect of Berberine (BBR) (15-45 μM) on protein expression levels in IL-21 (20 ng/mL) stimulated AA-FLS cells. Western blot analysis of PI3K, mTOR, IL-23 and PTEN are estimated in whole cell lysates using densitometry analysis. Comparisons are made with: FLS versus AA-FLS+IL-21+BBR (15-45 μM)/LY294002 (20 μM).

: LY294002 purchased from MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Apr;22(7):2005-2014. [Abstract]; Western blot detection of p-AKT and Bcl-2 protein expressions in brain tissue. LY294002 treatment apparently alleviates PI3K/AKT signaling pathway activity, Bcl-2, and VEGF protein expressions.

: LY294002 purchased from MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Aug;22(16):5377-5384. [Abstract]; Western blot shows that L-NBP pretreatment significantly up-regulates p-AKT and Bcl2 protein contents in HT22 cells induced by I/R, whereas LY294002 intervention markedly alleviates the influence of L-NBP on p-AKT and Bcl-2 expressions.

: LY294002 purchased from MedChemExpress. Usage Cited in: Food Nutr Res. 2018 Oct 12;62. [Abstract]; Western blotting of the PI3K/Akt signaling and the fold activation data analysis.

: LY294002 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 18;503(4):3212-3218. [Abstract]; Western blot analysis for phospho-PI3K, total PI3K, phospho-Akt, total Akt, phospho-mTOR and total mTOR in control/Brg^fl/fl+NS, control/Brg^fl/fl+LY294002 group, SFTPC-Cre/Brg^fl/fl+LY294002 and SFTPC-Cre/Brg^fl/fl+NS group.

: LY294002 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Apr;15(4):5685-5693. [Abstract]; HeLa cells are treated with GST S100A6 and LY294002 for 72 h, and total Akt, total GSK3β, β catenin, p Akt and p GSK3β are detected using western blotting

: LY294002 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2019 Jan;17(1):1372-1378. [Abstract]; Pretreatment of C666-1 cells with the phosphatidylinositol 3-kinase/Akt inhibitor LY294002 counteracts the triptolide‑induced inhibition of proliferation and apoptosis.

: LY294002 purchased from MedChemExpress. Usage Cited in: Exp Neurobiol. 2018 Dec;27(6):472-488. [Abstract]; LY294002 aggravates the suppression of PI3K/AKT signaling pathway induced by MEHP. CGCs are pre-treated with 5 μM of LY294002, an inhibitor of PI-3K/AKT pathway, for 2 h followed by treatment with 250 MEHP for 24 h.

: LY294002 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;51(4):1566-1583. [Abstract]; The protein expressions of PI3K, p-PI3K, Akt, p-Akt, Bax, Bcl-2, Cleaved-caspase-3, Caspase-3, are measured by Western blotting with the treatment of LY294002, CDDP or Icariin.

: LY294002 purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498. [Abstract]; Western blot analysis of AKT, p-Akt, mTOR, p-mTOR, FOXO1 and p-FOXO1 expression in U-87 MG cells after treatment with LY294002 (20 μM), Rapamycin (50 nM) or NAC (5 mM) with or without Xihuang pill (XHP).

: LY294002 purchased from MedChemExpress. Usage Cited in: Journal of Nanjing Agricultural University. 2018, 41(4): 708-714.; Effects of PI3K inhibitors on the expression of Cdc2, Cdc25B and CyclinB1 in sertoli cells.

: LY294002 purchased from MedChemExpress. Usage Cited in: Environ Pollut. 2017 Oct;229:964-975. [Abstract]; Inhibition of PI3K/AKT blocks MC-LR-induced NF-κB activation. SC, LC, and GC are pretreated with the PI3K/AKT inhibitor LY294002 (LY) at 20 μM for 1 h followed by a 6-h treatment with MC-LR. Expression of phosphorylated NF-κB p65 (p-p65) and total p65 are detected by western blotting.

: LY294002 purchased from MedChemExpress. Usage Cited in: Exp Gerontol. 2017 Dec 15;100:77-86. [Abstract]; Cells are treated with LY294002 5 μM for 2 h followed by treated with MANF 200 ng/mL for another 12 h, and then cell lysates are immunoblotted to assess the phosphorylation of Akt, GSK3β, and Nrf2.

: LY294002 purchased from MedChemExpress. Usage Cited in: Bosn J Basic Med Sci. 2017 May 20;17(2):132-137. [Abstract]; Effects of Akt/adenosine monophosphate-activated protein kinaseon CGP 48933 (VAL)-mediated endothelial nitric oxide (NO) synthase (eNOS) phosphorylation and NO production in human umbilical vein endothelial cells (HUVECs). (A) The variation of VAL (10 μM)-induced eNOS activation after HUVECs are incubated with LY294002 [LY] (10 μM), Compound C (1 μM), L-NAME (500 μM) for 3 hours. (B)The variation of VAL (10 μM)-induced nitric oxide (NO) productionafter HUVECs are incubated with LY294002 (10 μM),

: LY294002 purchased from MedChemExpress. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386; Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

: LY294002 purchased from MedChemExpress. Usage Cited in: J Cancer. 2016 Jun 5;7(9):1114-24. [Abstract]; Effects of PI3K inhibition. (A) Protein levels of p-AKT^S473 . (B) Inhibition of PI3K dose-dependently decreased the levels of p-EphA2^S897 in vitro.

: LY294002 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;40(3-4):579-588. [Abstract]; LY294002, a highly selective AKT inhibitor, completely blocks GSK3β phosphorylation induced by SDT. Effect of SDT on the expression of p-SMAD3, p-AKT and p-GSK3β. Images of p-GSK3β, GSK3β and GAPDH protein and mean values of protein level (relative to GAPDH) in cells.

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CK1 CK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

LY294002 is a broad-spectrum inhibitor of PI3K with IC₅₀s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively^[1]. LY294002 also inhibits CK2 with an IC₅₀ of 98 nM^[2]. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC₅₀ of 1.4?μM. LY294002 is an apoptosis activator^[3].

IC₅₀ & Target^[1]^[2]^[4]

p110α

0.5 μM (IC₅₀)

p110δ

0.57 μM (IC₅₀)

p110β

0.97 μM (IC₅₀)

human CK2

98 nM (IC₅₀)

human CK2α2

3.869 μM (IC₅₀)

DNA-PK

1.4 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
184B5	GI₅₀	29.37 μM Compound: 11, LY-294002	Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay Cytotoxicity against human 184B5 cells at 20 uM chloroquine by SRB assay	[PMID: 18691894]
184B5	GI₅₀	32.37 μM Compound: 11, LY-294002	Cytotoxicity against human 184B5 cells at 10 uM chloroquine by SRB assay Cytotoxicity against human 184B5 cells at 10 uM chloroquine by SRB assay	[PMID: 18691894]
184B5	GI₅₀	39.37 μM Compound: 11, LY-294002	Cytotoxicity against human 184B5 cells by SRB assay Cytotoxicity against human 184B5 cells by SRB assay	[PMID: 18691894]
786-0	IC₅₀	18.1 μM Compound: 1, LY294002	Inhibition of human 786-O cell proliferation after 72 hrs by spectrophotometric analysis Inhibition of human 786-O cell proliferation after 72 hrs by spectrophotometric analysis	[PMID: 23410005]
A549	IC₅₀	17.7 μM Compound: Ly; LY294002	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00603A
A549	IC₅₀	8.4 μM Compound: LY-294002	Antiproliferative activity against human A375 cells after 46 hrs Antiproliferative activity against human A375 cells after 46 hrs	[PMID: 17049248]
A549	IC₅₀	82.32 μM Compound: LY294002	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
A549	IC₅₀	82.32 μM Compound: LY294002	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31029551]
A549	IC₅₀	82.32 μM Compound: LY294002	Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay	[PMID: 25693787]
A549	IC₅₀	89.65 μM Compound: LY294002	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	10.1039/C2MD00255H
A549	IC₅₀	89.65 μM Compound: 3, LY-294002	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 22480851]
A549	IC₅₀	89.65 μM Compound: LY-294002	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 21945250]
BT-474	IC₅₀	20.7 μM Compound: 1, LY294002	Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis	[PMID: 23410005]
HCT-116	IC₅₀	5.3 μM Compound: 1, LY-294002	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay	[PMID: 22212721]
HCT-116	IC₅₀	5.8 μM Compound: 1, LY-294002	Growth inhibition of human HCT116 cells after 48 hrs by MTT assay Growth inhibition of human HCT116 cells after 48 hrs by MTT assay	[PMID: 22212721]
HCT-116	IC₅₀	51.82 μM Compound: LY294002	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
HCT-116	IC₅₀	51.82 μM Compound: LY294002	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31029551]
HCT-116	IC₅₀	51.82 μM Compound: LY294002	Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay	[PMID: 25693787]
HCT-116	IC₅₀	56.01 μM Compound: LY294002	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	10.1039/C2MD00255H
HCT-116	IC₅₀	56.01 μM Compound: 3, LY-294002	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 22480851]
HCT-116	IC₅₀	56.01 μM Compound: LY-294002	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 21945250]
HCT-116	IC₅₀	6.7 μM Compound: 1, LY-294002	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay	[PMID: 22212721]
HEK-293T	IC₅₀	0.42 μM Compound: LY294002	Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis	[PMID: 28280261]
HEK-293T	IC₅₀	1.53 μM Compound: LY294002	Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis	[PMID: 28280261]
HEK-293T	IC₅₀	10.3 μM Compound: LY294002	Inhibition of immobilized N-LY294002 bead binding to BRD2 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis Inhibition of immobilized N-LY294002 bead binding to BRD2 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis	[PMID: 28280261]
HEK-293T	IC₅₀	12.4 μM Compound: LY294002	Inhibition of immobilized N-LY294002 bead binding to C-terminal Flag-tagged BRD4 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis Inhibition of immobilized N-LY294002 bead binding to C-terminal Flag-tagged BRD4 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis	[PMID: 28280261]
HEK-293T	IC₅₀	13.7 μM Compound: LY294002	Inhibition of immobilized N-LY294002 bead binding to BRD3 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis Inhibition of immobilized N-LY294002 bead binding to BRD3 (unknown origin) expressed in HEK293T cell nuclear extract incubated for 1 hr by LC-MS/MS analysis	[PMID: 28280261]
HEK-293T	IC₅₀	2.37 μM Compound: LY294002	Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis	[PMID: 28280261]
HeLa	EC₅₀	1.5 μM Compound: 15, LY-294002	Activity at PI3K in human HeLa cells by ELISA Activity at PI3K in human HeLa cells by ELISA	[PMID: 20092323]
HeLa	IC₅₀	20.5 μM Compound: Ly; LY294002	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00603A
HeLa	IC₅₀	3 μM Compound: LY-294002	Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot	[PMID: 17135248]
HL-60	IC₅₀	14 μM Compound: LY-294002	Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay	[PMID: 26945110]
HL-60	IC₅₀	18.43 μM Compound: LY294002	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
HL-60	IC₅₀	18.43 μM Compound: LY294002	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31029551]
HL-60	IC₅₀	18.43 μM Compound: LY294002	Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay	[PMID: 25693787]
HL-60	IC₅₀	9.94 μM Compound: LY294002	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	10.1039/C2MD00255H
HL-60	IC₅₀	9.94 μM Compound: 3, LY-294002	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 22480851]
HL-60	IC₅₀	9.94 μM Compound: LY-294002	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 21945250]
Huh-7	IC₅₀	67.18 μM Compound: LY294002	Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31446244]
Huh-7	IC₅₀	67.18 μM Compound: LY294002	Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HuH7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31029551]
Huh-7	IC₅₀	67.18 μM Compound: LY294002	Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay	[PMID: 25693787]
J774	IC₅₀	3.7 μM Compound: LY294002	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA	[PMID: 29726680]
J774	IC₅₀	5.1 μM Compound: LY294002	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA	[PMID: 29726680]
J774	IC₅₀	8.9 μM Compound: LY294002	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay	[PMID: 29726680]
Jurkat	IC₅₀	22 μM Compound: LY-294002	Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay	[PMID: 26945110]
K562	IC₅₀	38 μM Compound: LY-294002	Antiproliferative activity against human K562 cells measured after 3 days by MTS assay Antiproliferative activity against human K562 cells measured after 3 days by MTS assay	[PMID: 26945110]
KB	IC₅₀	44.76 μM Compound: 3, LY-294002	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 22480851]
KB	IC₅₀	44.76 μM Compound: LY-294002	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 21945250]
MCF7	GI₅₀	2.63 μM Compound: 11, LY-294002	Cytotoxicity against human MCF7 cells in presence of 20 uM chloroquine by SRB assay Cytotoxicity against human MCF7 cells in presence of 20 uM chloroquine by SRB assay	[PMID: 18691894]
MCF7	IC₅₀	29.1 μM Compound: Ly; LY294002	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00603A
MCF7	GI₅₀	3.08 μM Compound: 11, LY-294002	Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay	[PMID: 18691894]
MCF7	GI₅₀	3.16 μM Compound: 11, LY-294002	Cytotoxicity against human MCF7 cells by SRB assay Cytotoxicity against human MCF7 cells by SRB assay	[PMID: 18691894]
MDA-MB-231	IC₅₀	0.38 μM Compound: LY294002	Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay	[PMID: 28302401]
MDA-MB-231	IC₅₀	0.38 μM Compound: LY-294002	Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay	[PMID: 22804108]
MDA-MB-231	IC₅₀	0.38 μM Compound: LY294002	Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs	[PMID: 28009521]
MDA-MB-231	IC₅₀	0.38 μM Compound: LY294002	Antimigratory activity against EGF induced chemotaxis in human MDA-MB-231 cells preincubated for 24 hrs followed by EGF addition for 3.5 hrs by light microscopy Antimigratory activity against EGF induced chemotaxis in human MDA-MB-231 cells preincubated for 24 hrs followed by EGF addition for 3.5 hrs by light microscopy	[PMID: 27598237]
MDA-MB-231	GI₅₀	3.32 μM Compound: 11, LY-294002	Cytotoxicity against human MDA-MB-231 cells in presence of 20 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-231 cells in presence of 20 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-231	GI₅₀	4.35 μM Compound: 11, LY-294002	Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-231	GI₅₀	6.71 μM Compound: 11, LY-294002	Cytotoxicity against human MDA-MB-231 cells by SRB assay Cytotoxicity against human MDA-MB-231 cells by SRB assay	[PMID: 18691894]
MDA-MB-231	IC₅₀	9.7 μM Compound: Ly; LY294002	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C5MD00603A
MDA-MB-468	GI₅₀	10.4 μM Compound: 11, LY-294002	Cytotoxicity against human MDA-MB-468 cells by SRB assay Cytotoxicity against human MDA-MB-468 cells by SRB assay	[PMID: 18691894]
MDA-MB-468	GI₅₀	4.76 μM Compound: 11, LY-294002	Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay	[PMID: 18691894]
MDA-MB-468	GI₅₀	8.2 μM Compound: 11, LY-294002	Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay	[PMID: 18691894]
MG-63	IC₅₀	55.2 μM Compound: 22; LY294002	Antiproliferative activity against human MG63 cells after 48 hrs by MTT assay Antiproliferative activity against human MG63 cells after 48 hrs by MTT assay	[PMID: 28537720]
NCI-H1299	IC₅₀	11.1 μM Compound: 1, LY294002	Inhibition of human H1299 cell proliferation after 72 hrs by spectrophotometric analysis Inhibition of human H1299 cell proliferation after 72 hrs by spectrophotometric analysis	[PMID: 23410005]
Neutrophil	IC₅₀	0.4 μg/mL Compound: LY294002	Inhibition of FMLP/CB-induced superoxide anion generation in human neutrophils by ferricytochrome c reduction method Inhibition of FMLP/CB-induced superoxide anion generation in human neutrophils by ferricytochrome c reduction method	[PMID: 24997688]
Neutrophil	IC₅₀	0.4 μM Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced superoxide anion generation by spectrophotometry Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/CB-induced superoxide anion generation by spectrophotometry	[PMID: 26575215]
Neutrophil	IC₅₀	0.6 μg/mL Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by fMLP/CB-induction measure Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by fMLP/CB-induction measure	[PMID: 25434002]
Neutrophil	IC₅₀	0.92 μg/mL Compound: LY294002	Inhibition of FMLP/CB-induced elastase release in human neutrophils after 5 mins by spectrophotometry Inhibition of FMLP/CB-induced elastase release in human neutrophils after 5 mins by spectrophotometry	[PMID: 24997688]
Neutrophil	IC₅₀	1 μM Compound: LY294002	Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry	[PMID: 24798144]
Neutrophil	IC₅₀	1.09 μM Compound: LY-294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced superoxide anion production after 5 mins by spectrophotometer analysis Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced superoxide anion production after 5 mins by spectrophotometer analysis	[PMID: 21391659]
Neutrophil	IC₅₀	1.12 μM Compound: LY-294002	Antiinflammatory activity against human neutrophil assessed as inhibition of N-formyl-l-methionyl phenylalanine/cytochalasin B-induced superoxide anion generation by spectrophotometry Antiinflammatory activity against human neutrophil assessed as inhibition of N-formyl-l-methionyl phenylalanine/cytochalasin B-induced superoxide anion generation by spectrophotometry	[PMID: 21316977]
Neutrophil	IC₅₀	1.12 μM Compound: LY294002	Antiinflammatory activity in FMLP/CB activated human neutrophils assessed as inhibition of superoxide generation by ferricytochrome c reduction based spectrophotometry Antiinflammatory activity in FMLP/CB activated human neutrophils assessed as inhibition of superoxide generation by ferricytochrome c reduction based spectrophotometry	[PMID: 23347584]
Neutrophil	IC₅₀	1.2 μg/mL Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction by spectroscopic analysis Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction by spectroscopic analysis	[PMID: 25434002]
Neutrophil	IC₅₀	1.25 μM Compound: LY294002	Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation pretreated for 5 mins followed by cytochalasin B addition for 3 mins and subsequent fMLP stimulation for 10 mins by superoxide dismutase Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation pretreated for 5 mins followed by cytochalasin B addition for 3 mins and subsequent fMLP stimulation for 10 mins by superoxide dismutase	[PMID: 29381070]
Neutrophil	IC₅₀	1.5 μM Compound: LY294002	Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins	[PMID: 24798144]
Neutrophil	IC₅₀	1.8 μM Compound: LY294002	Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced superoxide anion generation preincubated for 5 mins followed by CB stimulation for 3 mins and subsequent fMLF stimulation for 10 mins by spectrophotometric method Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced superoxide anion generation preincubated for 5 mins followed by CB stimulation for 3 mins and subsequent fMLF stimulation for 10 mins by spectrophotometric method	[PMID: 28445049]
Neutrophil	IC₅₀	1.98 μM Compound: LY-294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate after 5 mins Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate after 5 mins	[PMID: 21391659]
Neutrophil	IC₅₀	2.1 μM Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation preincubated for 5 mins followed by cytochalasin B/fMLP addition for 3 mins by superoxide dismutase inhibitable reduction of ferricytochro Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation preincubated for 5 mins followed by cytochalasin B/fMLP addition for 3 mins by superoxide dismutase inhibitable reduction of ferricytochro	[PMID: 29975532]
Neutrophil	IC₅₀	3.3 μM Compound: LY294002	Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced elastase release by measuring degranulation of azurophilic granules using MeOSuc-Ala-Ala-ProVal-p-nitroanilide as substrate preincubated for 5 mins followed by CB/fM Anti-inflammatory activity in human neutrophils assessed as inhibition of fMLF/CB-induced elastase release by measuring degranulation of azurophilic granules using MeOSuc-Ala-Ala-ProVal-p-nitroanilide as substrate preincubated for 5 mins followed by CB/fM	[PMID: 28445049]
Neutrophil	IC₅₀	3.44 μM Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release pretreated for 5 mins followed by fMLP/CB stimulation using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release pretreated for 5 mins followed by fMLP/CB stimulation using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate	[PMID: 29381070]
Neutrophil	IC₅₀	3.65 μM Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation after 5 mins by ferricytochrome c based spectrophotometric analysis Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation after 5 mins by ferricytochrome c based spectrophotometric analysis	[PMID: 27256910]
Neutrophil	IC₅₀	5.1 μM Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release preincubated for 5 mins followed by fMLP/CB stimulation and measured for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release preincubated for 5 mins followed by fMLP/CB stimulation and measured for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate	[PMID: 29975532]
Neutrophil	IC₅₀	5.15 μM Compound: LY294002	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate after 5 mins by spectrofluorometric analysis Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate after 5 mins by spectrofluorometric analysis	[PMID: 27256910]
OVCAR-3	IC₅₀	9.19 μM Compound: LY294002	Cytotoxicity against human OVCAR-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Blue cell viability assay Cytotoxicity against human OVCAR-3 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Blue cell viability assay	[PMID: 35100504]
PBMC	IC₅₀	> 50 μM Compound: LY-294002	Cytotoxicity against PHA induced human PBMC after 3 days by MTS assay Cytotoxicity against PHA induced human PBMC after 3 days by MTS assay	[PMID: 26945110]
PC-3	IC₅₀	1.3 μM Compound: 1, LY294002	Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA	[PMID: 23410005]
PC-3	IC₅₀	12.1 μM Compound: 1, LY294002	Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis	[PMID: 23410005]
PC-3	IC₅₀	61.35 μM Compound: LY294002	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	10.1039/C2MD00255H
PC-3	IC₅₀	61.35 μM Compound: 3, LY-294002	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 22480851]
PC-3	IC₅₀	61.35 μM Compound: LY-294002	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 21945250]
Sf21	IC₅₀	0.5 μM Compound: LY-294002	Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging	[PMID: 22520630]
Sf21	IC₅₀	0.97 μM Compound: LY-294002	Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging	[PMID: 22520630]
Sf9	IC₅₀	0.34 μM Compound: LY-294002	Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.55 μM Compound: 3	Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay	[PMID: 21121631]
Sf9	IC₅₀	0.63 μM Compound: LY-294002	Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	1.6 μM Compound: LY-294002	Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	2.1 μM Compound: LY-294002	Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
U-266	IC₅₀	46 μM Compound: LY-294002	Antiproliferative activity against human U266 cells measured after 3 days by MTS assay Antiproliferative activity against human U266 cells measured after 3 days by MTS assay	[PMID: 26945110]
U2OS	IC₅₀	62.96 μM Compound: 22; LY294002	Antiproliferative activity against human U2OS cells after 48 hrs by MTT assay Antiproliferative activity against human U2OS cells after 48 hrs by MTT assay	[PMID: 28537720]
U-87MG ATCC	IC₅₀	8.1 μM Compound: LY-294002	Inhibition of GSK3-beta in human U87MG cells by ELISA Inhibition of GSK3-beta in human U87MG cells by ELISA	[PMID: 18345609]
U-937	IC₅₀	14 μM Compound: LY-294002	Antiproliferative activity against human U937 cells measured after 3 days by MTS assay Antiproliferative activity against human U937 cells measured after 3 days by MTS assay	[PMID: 26945110]

In Vitro

LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion^[4].
LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent^[4].
LY294002 (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration^[4].
LY294002 (5, 10, 100 μM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 μM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[4]

Cell Line:	CNE-2Z cells
Concentration:	0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
Incubation Time:	24 hours and 48 hours
Result:	Decreased CNE-2Z cells in a dose-dependent fashion.

Apoptosis Analysis^[4]

Cell Line:	CNE-2Z cells
Concentration:	0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
Incubation Time:	24 hours and 48 hours
Result:	Induced apoptosis rate in dose-dependent.

Western Blot Analysis^[4]

Cell Line:	CNE-2Z cells
Concentration:	10 μM, 25 μM, 50 μM, and 75 μM
Incubation Time:
Result:	Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group.

In Vivo

LY294002 (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden^[4].
LY294002 (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Athymic nude mice (6-8 weeks) with CNE-2Z xenograft^[4]
Dosage:	10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg
Administration:	Intraperitoneal injection; twice weekly, for 4 weeks
Result:	Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.

Molecular Weight

307.34

Formula

C₁₉H₁₇NO₃

CAS No.

154447-36-6

Appearance

Solid

Color

White to yellow

SMILES

O=C1C=C(OC2=C1C=CC=C2C3=CC=CC=C3)N4CCOCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (162.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (162.69 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2537 mL	16.2686 mL	32.5373 mL
5 mM	0.6507 mL	3.2537 mL	6.5075 mL
10 mM	0.3254 mL	1.6269 mL	3.2537 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.87 mg/mL (9.34 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 15.71 mg/mL (51.12 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (285 KB) SDS (392 KB)

COA (254 KB) HNMR (172 KB) LCMS (372 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[1]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms. Biochem J. 2007 Jun 15;404(3):449-58. [Content Brief]

[2]. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21. [Content Brief]

[3]. Davidson D, et al. Small Molecules, Inhibitors of DNA-PK, Targeting DNA Repair, and Beyond. Front Pharmacol. 2013 Jan 31;4:5. [Content Brief]

[4]. Jiang H, et al. Phosphatidylinositol 3-kinase inhibitor(LY294002) induces apoptosis of human nasopharyngeal carcinoma invitro and in vivo. J Exp Clin Cancer Res. 2010 Apr 22;29:34. [Content Brief]

[5]. Md Mokhtar AH, et al. LY294002, a PI3K pathway inhibitor, prevents leptin-induced adverse effects on spermatozoa in Sprague-Dawley rats. Andrologia. 2019 Apr;51(3):e13196. [Content Brief]

[6]. Yi-Jen Hsueh, et al. Lysophosphatidic acid induces YAP-promoted proliferation of human corneal endothelial cells via PI3K and ROCK pathways. Mol Ther Methods Clin Dev. 2015 Apr 29;2:15014. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	3.2537 mL	16.2686 mL	32.5373 mL	81.3431 mL
	5 mM	0.6507 mL	3.2537 mL	6.5075 mL	16.2686 mL
	10 mM	0.3254 mL	1.6269 mL	3.2537 mL	8.1343 mL
	15 mM	0.2169 mL	1.0846 mL	2.1692 mL	5.4229 mL
	20 mM	0.1627 mL	0.8134 mL	1.6269 mL	4.0672 mL
	25 mM	0.1301 mL	0.6507 mL	1.3015 mL	3.2537 mL
	30 mM	0.1085 mL	0.5423 mL	1.0846 mL	2.7114 mL
	40 mM	0.0813 mL	0.4067 mL	0.8134 mL	2.0336 mL
	50 mM	0.0651 mL	0.3254 mL	0.6507 mL	1.6269 mL
	60 mM	0.0542 mL	0.2711 mL	0.5423 mL	1.3557 mL
	80 mM	0.0407 mL	0.2034 mL	0.4067 mL	1.0168 mL
	100 mM	0.0325 mL	0.1627 mL	0.3254 mL	0.8134 mL

LY294002 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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LY294002

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LY294002

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Other Forms of LY294002:

LY294002 Related Antibodies

780 Publications Citing Use of MCE LY294002

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Casein Kinase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

LY294002 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

LY294002 Related Classifications

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Your Recently Viewed Products:

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