LY294002

別名：SF 1101, NSC 697286

製品コード：S1105 純度：99.99%

LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKｃｓ を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。

CAS No. 154447-36-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 28600	国内在庫あり
10mg	JPY 22000	国内在庫あり
25mg	JPY 40500	国内在庫あり
200mg	JPY 115500	国内在庫あり
1g	JPY 220500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（1583）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

LY294002関連製品

関連ターゲット	p110α p110β p110δ p110γ C2β Vps34	もっと見る
関連製品	3-MA (3-Methyladenine) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147) TG100-115 CZC24832 Voxtalisib (XL765) XL147 analogue AS-604850 BGT226 (NVP-BGT226) maleate Quercetin Dihydrate VPS34 inhibitor 1 (Compound 19) Samotolisib (LY3023414) Voxtalisib (XL765) Analogue AMG319 Nemiralisib Bimiralisib (PQR309) CH5132799 PKI-402 TG100713 Paxalisib (GDC-0084) SF2523 Serabelisib (TAK-117) GDC-0326 GNE-317 Inavolisib (GDC-0077) PIK-294 PI-3065 AZD8835 Seletalisib (UCB-5857) leniolisib (CDZ 173) (E)-Akt inhibitor-IV Gallein CAY10505 Selective PI3Kδ Inhibitor 1 (compound 7n) PF-4989216 GNE-477 GNE-493	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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 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
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 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 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 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
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	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	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
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
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 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 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
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
MCF7 cells	Function assay	10 uM	1 hr	Inhibition of IGF1R phosphorylation at Tyr1161 residue in human MCF7 cells at 10 uM after 1 hr by Hoechst 33258 staining based immunohistochemical analysis	28557430
SKOV3 cells	Function assay	20 uM	24 hrs	Inhibition of BDNF-induced invasion in human SKOV3 cells at 20 uM after 24 hrs in by matrigel invasion assay	29122484
SKOV3 cells	Antimigratory assay	20 uM	24 hrs	Antimigratory activity against human SKOV3 cells assessed as inhibition of BDNF-induced cell migration at 20 uM after 24 hrs by scratch wound healing assay	29122484
J774 cells	Function assay	10 uM	4 hrs	Inhibition of PI3K/Akt in mouse J774 cells assessed as reduction in LPS-induced Akt phosphorylation at Ser473 at 10 uM after 4 hrs by Western blot analysis	29726680
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 HCT116 cells	Function assay	10 μM		Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis	22212721
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
mouse mast cells	Function assay	20 μM		Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM	16789742
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
human KB cells	Cytotoxic assay		72 h	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM.	21945250
human HCT116 cells	Cytotoxic assay		72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM.	21945250
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
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 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 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 A375 cells	Proliferation assay		46 h	Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM.	17049248
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
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 A549 cells	Cytotoxic assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	22480851
human PC3 cells	Cytotoxic assay		72 h	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM.	22480851
human HL60 cells	Cytotoxic assay		72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM.	22480851
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
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
human BT474 cell	Proliferation assay		72 h	Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis， IC50=20.7 μM.	23410005
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 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
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 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 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 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
HL60 cells	Antiproliferative assay		3 days	Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay, IC50 = 14 μM.	26945110
U937 cells	Antiproliferative assay		3 days	Antiproliferative activity against human U937 cells measured after 3 days by MTS assay, IC50 = 14 μM.	26945110
Jurkat cells	Antiproliferative assay		3 days	Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay, IC50 = 22 μM.	26945110
K562 cells	Antiproliferative assay		3 days	Antiproliferative activity against human K562 cells measured after 3 days by MTS assay, IC50 = 38 μM.	26945110
U266 cells	Antiproliferative assay		3 days	Antiproliferative activity against human U266 cells measured after 3 days by MTS assay, IC50 = 46 μM.	26945110
MDA-MB-231 cells	Antimigratory assay		24 hrs	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, IC50 = 0.38 μM.	27598237
MDA-MB-231 cells	Antiinvasive assay		3.5 hrs	Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs, IC50 = 0.38 μM.	28009521
HEK293T cells	Function assay		1 hr	Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 0.42 μM.	28280261
HEK293T cells	Function assay		1 hr	Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 1.53 μM.	28280261
HEK293T cells	Function assay		1 hr	Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 2.37 μM.	28280261
J774 cells	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA, IC50 = 3.7 μM.	29726680
J774 cells	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA, IC50 = 5.1 μM.	29726680
J774 cells	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 8.9 μM.	29726680
Sf9 cells	Fluorescent polarization assay			Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM.	21121631
Sf9 cells	fluorescent polarization assay			Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay	21121631
Sf21 cells	Function assay			Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM.	19748269
human MCF7 cells	Cytotoxic assay			Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM.	18691894
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
MDA-MB-231 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM.	18691894
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 MDA-MB-468 cells	Cytotoxic assay			Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM.	18691894
human 184B5 cells	Cytotoxic assay			Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM.	18691894
human U251HRE cells	Function assay			Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay	18501601
human U87MG cells	Function assay			Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM.	18345609
rat RBL2H3 cells	Function assay			Inhibition of A23187-induced degranulation in rat RBL2H3 cells	18328716
Sf9 cells	Function assay			Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM.	18321716
human A375 cells	Proliferation assay			Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM.	17601739
HeLa cells	Function assay			Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM.	17135248
THP1 cells	Function assay			Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM.	16789742
THP1 cells	Function assay			Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM.	16789742
mouse Raw264 macrophage	Function assay			Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM.	16789742
THP1 cells	Function assay			Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM.	16789742
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
HeLa cells	Binding affinity assay			Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM	15658870
HeLa cells	Function assay			Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM.	15658870
Sf9 cells	Function assay			Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM.	10998351
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
Sf9 cells	Function assay			Inhibition of His-tagged human CK2 expressed in Sf9 cells, IC50 = 6.9 μM.	10998351
HeLa cells	Function assay			In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells., IC50 = 1.4 μM.	12941339
HeLa cells	Function assay			Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50 = 1.5 μM.	15658870
Sf21 cells	Function assay			Inhibition of human recombinant PI3Kbeta expressed in baculovirus-infected Sf21 cells, IC50 = 0.9 μM.	19748269
Sf21 cells	Function assay			Inhibition of bovine recombinant PI3Kgamma expressed in baculovirus-infected Sf21 cells, IC50 = 7 μM.	19748269
HeLa cells	Function assay			Activity at PI3K in human HeLa cells by ELISA, EC50 = 1.5 μM.	20092323
Sf21 cells	Function assay			Inhibition of PI3Kdelta expressed in cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.57 μM.	22520630
Sf21 cells	Function assay			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, IC50 = 0.97 μM.	22520630
MDA-MB-231 cells	Function assay			Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay, IC50 = 0.38 μM.	28302401
NB1643 cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50 cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2 cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC cells	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
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生物活性

製品説明

Targets

CK2 ^[5] (Cell-free assay)	p110α ^[1] (Cell-free assay)	p110δ ^[1] (Cell-free assay)	p110β ^[1] (Cell-free assay)	DNA-PK ^[6] (Cell-free)
98 nM	0.5 μM	0.57 μM	0.97 μM	1.4 μM

In Vitro
In vitro	LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1^[5]. 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]
Kinase Assay	kinase assays
Kinase Assay	PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24^oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.
細胞実験	細胞株	Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
	濃度	0–50 μM
	反応時間	0–48 hours
	実験の流れ	1.0×10⁵ cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37^oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37^oC, after which absorbance at 450 nm is measured with a microplate reader.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	E-cadherin / p-Akt / Akt beta-catenin / p-GSK3β / Cyclin D1 Bcl-xl / Bax / caspase3 / cleaved caspase-3 p-p70S6K (T389) / p-GSK3β(S9) / pERK / Vinculin pPKB-S473		29731993
	Growth inhibition assay	Cell viability		25344912
	Immunofluorescence	α-SMA / CD31 E-cadherin / beta-catenin COX-2 / p-NFκB FOXO3a		27671604
	ELISA	IL-10 / IL-1β / TNFα / IL-6		22208359

In Vivo
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]
動物実験	動物モデル	Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
	投与量	0–100 mg/kg
	投与経路	Administered via i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02337309	Terminated	Neuroblastoma	New Approaches to Neuroblastoma Therapy Consortium\|SignalRX Pharmaceuticals Inc.\|University of Southern California	July 9 2015	Phase 1

参考
[1] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58. [2] Semba S, et al. Clin Cancer Res, 2002, 8(6), 1957-63. [3] Hu L, et al. Clin Cancer Res, 2000, 6(3), 880-6. [4] Gharbi SI, et al. Biochem J, 2007, 404(1), 15-21. [5] Severine I. Gharbi, et al. Biochem J. 2007, 404(3):449-58. [6] David Davidson, et al. Front Pharmacol. 2013, 4: 5. + 展開

参考

+ 展開

化学情報

分子量	307.34	化学式	C₁₉H₁₇NO₃
CAS No.	154447-36-6	SDF	Download LY294002 SDFをダウンロードする
Smiles	C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 61 mg/mL ( (198.47 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 15 mg/mL

Water : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.4mg/ml (11.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 68 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%absolute ethyl alcohol 1 95%Corn oil	1.0mg/ml (3.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear absolute ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.0mg/ml (9.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問（FAQ）

質問1:
I want to buy a inhibitor that can inactivates Akt/PI3K. I notice the protocol of LY294002 (catalog no. s1105) says it will inactivates Akt/PKB. Is LY294002 available for Akt/PI3K inhibition?

回答
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively. It can inhibit PI3K/AKT. PKB is the alternative name of AKT.

質問2:
What is the suggested formulation of this compound for mouse injection(i.p.)?

回答
It can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly, and the concentration of DMSO is safe for in vivo experiments.

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