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Reagents and instruments for immunology, cell biology and molecular biology.

LY294002 [154447-36-6]

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Cat# HY-10108-10mg

Size : 10mg

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Brand : MedChemExpress

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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.

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: 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 2

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 3

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

Purity & Documentation

Purity: 99.95%

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]

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