Welcome to SuperLan Chemical Co.,Ltd.
Home > Products > PI3K/Akt/mTOR > PI3K > LY294002

LY294002

(CAS No:154447-36-6)
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
CAS No:154447-36-6
Molecular Weight(MW):307.34
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
Price and large packaging, please e-mail consultation:info@SuperLan-chem.com
QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 154447-36-6
Molecular formula(MF) C19H17NO3
Molecular Weight(MW): 307.34
Alias LY 294002 hydrochloride
Solubility
In vitro DMSO 36 mg/mL (117.13 mM)
Ethanol 21 mg/mL (68.32 mM)
Water <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL
Biological Activity
Description LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
Targets
p110α [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)
0.5 μM 0.57 μM 0.97 μM
In vitro

LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells Cell invasion assay 24 h Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay, IC50=0.38 μM. 22804108
Sf21 cells Function assay 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, IC50=0.5 μM 22520630
Sf21 cells Function assay Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM. 19748269
Sf9 cells Fluorescent polarization assay Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM. 21121631
THP1 cells Function assay Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM. 16789742
human PC3 cells Function assay 30 min Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA, IC50=1.3μM. 23410005
HeLa (human carcinoma) cells. Function assay In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM. 15658870
THP1 cells Function assay Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM. 16789742
HeLa cells Function assay Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM. 15658870
human MCF7 cells Cytotoxic assay Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM. 18691894
HeLa cells Function assay Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM. 17135248
human MCF7 cells Cytotoxic assay Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=3.08 μM. 18691894
human MCF7 cells Cytotoxic assay Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 μM. 18691894
human MDA-MB-231 cells Cytotoxic assay Cytotoxicity against human MDA-MB-231 cells in presence of 20 μM chloroquine by SRB assay, GI=3.32 μM. 18691894
human MDA-MB-231 cells Cytotoxic assay Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.35 μM. 18691894
human MDA-MB-468 cells Cytotoxic assay Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay， IC50=4.76 μM. 18691894
human HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM 22212721
human HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=5.8 μM. 22212721
HeLa cells Binding affinity assay Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM 15658870
human HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=6.7 μM. 22212721
MDA-MB-231 cells Cytotoxic assay Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM. 18691894
Sf9 cells Function assay Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM. 18321716
human U87MG cells Function assay Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM. 18345609
human MDA-MB-468 cells Cytotoxic assay Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=8.2 μM. 18691894
human A375 cells Proliferation assay 46 h Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM. 17049248
human A375 cells Proliferation assay Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM. 17601739
human HL60 cells Cytotoxic assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM. 22480851
mouse Raw264 macrophage Function assay Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM. 16789742
Sf9 cells Function assay Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM. 10998351
human MDA-MB-468 cells Cytotoxic assay Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM. 18691894
human PC3 cell Proliferation assay 72 h Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=12.1 μM. 23410005
human HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=18.43 μM. 25693787
human BT474 cell Proliferation assay 72 h Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis， IC50=20.7 μM. 23410005
THP1 cells Function assay Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM. 16789742
human 184B5 cells Cytotoxic assay Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM. 18691894
human KB cells Cytotoxic assay 72 h Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM. 21945250
mouse RAW264.7 cells Function assay 25 μM 20 h Inhibition of PI3K/AKT in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS protein expression at 25 μM after 20 hrs by Western blot analysis 24299616
human A2780 cells Apoptosis assay 2 μM 12 h Induction of apoptosis in cisplatin-resistant human A2780 cells assessed as decrease in phosphorylated Akt level at 2 uM after 12 hrs by immunoblot analysis. 17684018
human SW480 cells Function assay 20 μM 24 h Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis 17472962
mouse mast cells Function assay 20 μM Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM 16789742
human BJ cells Function assay 25 μM 2 h Inhibition of PI3K signaling in PDGF-stimulated serum starved human BJ cells transfected with plasmid EGFP/PH domain of Akt assessed as suppression of PH-EGFP redistribution to plasma membrane at 25 uM treated 2 hrs before PDGF challenge by confocal microscopy 16767085
human IGROV1 cells Function assay 24/48 h Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in phosphorylated AKT level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis 21216151
human IGROV1 cells Function assay 24/48 h Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in cyclin D1 level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis 21216151
rat RBL2H3 cells Function assay Inhibition of A23187-induced degranulation in rat RBL2H3 cells 18328716
human BJ cells Function assay 25 μM 2 h Activation of Akt phosphorylation at Thr308 in PDGF-stimulated serum starved human BJ cells at 25 uM treated 2 hrs before PDGF challenge by immunoblotting 16767085
human HCT116 cells Function assay 10 μM 10 min Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins 22212721
human HCT116 cells Function assay 10 μM 10 min Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins 22212721
human HCT116 cells Function assay 10 μM Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis 22212721
human HCT116 cells Function assay 10 μM Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis 22212721
human PC3 cells Function assay 50 μM 8 h Induction of p21 protein expression in human PC3 cells at 50 uM incubated for 8 hrs by Western blotting relative to untreated control 22998472
human LNCAP cells Function assay 0.1-30 μM 30 min Inhibition of Akt phosphorylation in human LNCAP cells at 0.1 to 30 uM after 30 mins by Western blot analysis 22832316
human LNCAP cells Function assay 0.1-30 μM 24 h Downregulation of survivin expression in human LNCAP cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22832316
HUVEC Function assay 10-25 μM 16 h Inhibition of TNFalpha-stimulated ICAM-1 mRNA expression in HUVEC at 10 to 25 uM pretreated for 16 hrs before TNFalpha challenge measured after 6 hrs by RT-PCR analysis 22026410
HUVEC Function assay 10-25 μM 30 min Inhibition of TNFalpha-stimulated human ICAM-1 promoter activity expressed in HUVEC assessed as beta-galactosidase activity at 10 to 25 uM pretreated for 30 mins before TNFalpha challenge measured after 5 hrs by luciferase reporter gene assay 22026410
human H1299 cells Function assay 0.1-30 μM 24 h Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22622069
human H1299 cells Function assay 0.1-30 μM 24 h Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis in presence of 100 ug/ml TRAIL and PI3K inhibitor LY294002 22622069
human H1299 cells Function assay 0.1-30 μM 24 h Induction of DR5 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22622069
human H1299 cells Function assay 0.1-30 μM 24 h Induction of JNK-mediated CHOP expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22622069
HEK293 cells Function assay 1.5 h Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting 22537153
human U251HRE cells Function assay Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay 18501601
human HCT116 cells Function assay 10 μM Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis 22212721
Sf9 cells fluorescent polarization assay Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay 21121631
human HCT116 cells Proliferation assay 72 h Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=51.82 μM. 25693787
human HCT116 cells Cytotoxic assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM. 21945250
human PC3 cells Cytotoxic assay 72 h Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM. 22480851
human HuH7 cells Proliferation assay 72 h Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=67.18 μM. 25693787
human A549 cells Proliferation assay 72 h Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=82.32 μM. 25693787
human A549 cells Cytotoxic assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay 22480851
human PC3 cells Proliferation assay 25 μM 120 h Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO 16680159
human H460 cells Function assay 30 μM Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM 18501601
human IGROV1 cells Function assay 24 h Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 1 fold IC50 after 24 hrs by flow cytometry 21216151
human IGROV1 cells Function assay 24 h Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 5 fold IC50 after 24 hrs by flow cytometry 21216151
human H4 cells Function assay 2 h Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control 18024584
human MGC803 cells Function assay 25 μM 48 h Cell cycle arrest in human MGC803 cells assessed as accumulation at G2/M phase at 25 uM after 48 hrs using propidium iodide staining after 48 hrs by flow cytometer relative to control 24119869

... Click to View More Cell Line Experimental Data
In vivo LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]
Copyright 2016 Shanghai Superlan Chemcial Technology Centre
Technical Support:chem960