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LY294002

カタログ番号 T2008   CAS 154447-36-6
別名: LY 294002, NSC 697286, SF 1101

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

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LY294002, CAS 154447-36-6
パッケージサイズ 在庫状況 単価(税別)
サンプルについてお問い合わせ
5 mg 在庫あり ￥ 8,000
10 mg 在庫あり ￥ 11,000
50 mg 在庫あり ￥ 16,000
100 mg 在庫あり ￥ 20,500
200 mg 在庫あり ￥ 30,000
1 mL * 10 mM (in DMSO) 在庫あり ￥ 12,500
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純度: 99.93%
COA DATASHEET SDS HNMR HPLC
純度: 99.92%
COA DATASHEET SDS HPLC HNMR
純度: 99.76%
COA DATASHEET SDS HNMR HPLC
純度: 99.76%
COA DATASHEET SDS
純度: 98%
COA DATASHEET SDS HNMR
純度: 98%
COA DATASHEET SDS HNMR
COA DATASHEET SDS HNMR
COA DATASHEET SDS
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生物学的特性に関する説明
化学的特性
保存条件 & 溶解度情報
説明 LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.
ターゲット＆IC50 p110α:0.5 μM (cell free), DNA-PK:1.4 μM (cell free), p110δ:0.57 μM (cell free), p110β:0.97 μM (cell free)
In vitro METHODS: Human pancreatic cancer cells AsPC-1, BxPC-3 and PANC-1 were treated with LY294002 (5-45 µM) for 24 h. Cell growth inhibition was detected by MTT.
RESULTS: LY294002 dose-dependently induced the growth of AsPC-1, BxPC-3 and PANC-1 cells with IC50 of 40 μM, 5 μM and 35 μM, respectively.[1]
METHODS: Chinese hamster ovary cells CHO-IR expressing human insulin receptor were treated with LY294002 (5 µM) for 5 min and stimulated with Insulin (1 nM, 10 min), and the expression levels of target proteins were detected by Western Blot.
RESULTS: LY294002 blocked insulin-induced phosphorylation of PKB Ser473 in CHO-I R cells. [2]
METHODS: Human nasopharyngeal carcinoma cells CNE-2Z were treated with LY294002 (10-75 μmol/L) for 24-48 h. Apoptosis was detected by Flow Cytometry.
RESULTS: LY294002 dose-dependently induced apoptosis in CNE-2Z cells. [3]
In vivo METHODS: To detect anti-tumor activity in vivo, LY294002 (25 mg/kg twice weekly) and cisplatin (5 mg/kg once weekly) were intraperitoneally injected into BALB/C nu/nu mice harboring human pancreatic cancer tumor AsPC-1 for three weeks.
RESULTS: Tumor volume increased in the control mice, while the cisplatin or LY294002 treatment groups showed a 77% and 70% reduction in tumor volume, respectively. The combination treatment group was more effective, with tumor volume growth decreasing to 44% of the control group's volume. [4]
METHODS: To investigate whether pharmacological blockade of PI3K could ameliorate the development of LPS-induced acute liver injury in mice, LY294002 (40 μM; 10 μL) was administered by single intraperitoneal injection to the LPS-induced acute hepatic injury BALB/c mouse model.
RESULTS: In LPS-induced hepatitis, LY294002 treatment markedly inhibited the intrahepatic synthesis of various disease-associated pro-inflammatory cytokines, including tumor necrosis factor-α, IL-6, IL-1β, and INF-γ. Significant inhibition of IκB phosphorylation was observed in liver samples from LPS-injured mice with LY294002. Therefore, LY294002 may protect the liver from LPS-induced injury by inhibiting the IκB nuclear factor κ light chain enhancer of the activated B cell-dependent signaling pathway. [5]
キナーゼ試験 PI3K inhibition by LY294002 was determined in a radiometric assay using purified, recombinant enzymes (class IA and class IB) with 1 μM ATP. The kinase reaction was carried out for 1 h at room temperature (24 °C) and was terminated by addition of PBS. IC50 values were subsequently determined using a sigmoidal dose-response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition were established by kinase selectivity screening. Inhibitor (10 μM; LY294002) was tested against the Upstate panel of kinases in 10 μM ATP [4].
細胞研究 The cells were seeded into 96-well plates at 5000 cells/well. Twenty-four hours after cells were seeded, the medium was removed and replaced in the presence of LY294002 (0 μmol/L, 10 μmol/L, 25 μmol/L, 50 μmol/L, and 75 μmol/L) dissolved in DMSO or DMSO only for an additional 24 h and 48 h. To avoid any nonspecific toxic effects of DMSO on cell growth, DMSO concentrations were maintained at 0.5% in all experiments. MTT dye (5 mg/mL) was added to each well. The reaction was stopped by the addition of DMSO, and optical density was measured at 490 nm on a multiwell plate reader. Background absorbance of the medium in the absence of cells was subtracted. All samples were assayed in triplicate, and the mean for each experiment was calculated. Results were expressed as a percentage of control, which was considered to be 100% [3].
動物実験 Athymic nude mice were used when they were 6-8 weeks. Mice were randomly divided into free separated into five groups (n = 4 mice). Mice were housed in the same environment with controlled temperature, humidity, and a 12 h light/dark cycle. Mice were inoculated subcutaneously with CNE-2Z cells (1 × 10^6 cells/mouse in 200 μl of RPMI-1640) into the flank. The tumor take rate was 100%. After 1 week, an intraperitoneal injection was performed to the xenograft mice with different dosage of LY294002 (10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg twice weekly (n = 4 mice), each group for 4 weeks. Treated mice have monitored any signs. Body weight and tumors size were measured twice a week. Tumor size was measured using calipers and tumor volume was calculated (volume = long axis × short axis^2). At the end of the treatment, all mice were euthanized. One part of tumor tissue was fixed in formalin and embedded in paraffin, and another part was stored at -70°C [3].
別名 LY 294002, NSC 697286, SF 1101
分子量 307.34
分子式 C19H17NO3
CAS No. 154447-36-6

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

Ethanol: 10 mg/mL(32.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 6.25 mg/mL (20.34 mM), Sonication is recommended.

参考文献

1. Mao Y, et al. Regulation of cell apoptosis and proliferation in pancreatic cancer through PI3K/Akt pathway via Polo-like kinase Oncol Rep. 2016 Jul;36(1):49-56. 2. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. 3. Jiang H, et al. Phosphatidylinositol 3-kinase inhibitor(LY294002) induces apoptosis of human nasopharyngeal carcinoma in vitro and in vivo. J Exp Clin Cancer Res. 2010 Apr 22;29(1):34. 4. Fujiwara M, et al. Modulating effect of the PI3-kinase inhibitor LY294002 on cisplatin in human pancreatic cancer cells. J Exp Clin Cancer Res. 2008 Nov 25;27(1):76. 5. Chen Z, et al. LY294002 prevents lipopolysaccharide‑induced hepatitis in a murine model by suppressing IκB phosphorylation. Mol Med Rep. 2016 Jan;13(1):811-6. 6. Wen Y, Peng D, Li C, et al. A new polysaccharide isolated from Morchella importuna fruiting bodies and its immunoregulatory mechanism[J]. International Journal of Biological Macromolecules. 2019, 137: 8-19. 7. Zhao Y, Guo W, Gu X, et al. Repression of deoxynivalenol-triggered cytotoxicity and apoptosis by mannan/β-glucans from yeast cell wall: Involvement of autophagy and PI3K-AKT-mTOR signaling pathway[J]. International Journal of Biological Macromolecules. 2020, 164: 1413-1421. 8. Gu L, Wang Y, Xu Y, et al. Lunasin functionally enhances LDL uptake via inhibiting PCSK9 and enhancing LDLR expression in vitro and in vivo[J]. Oncotarget. 2017 Aug 24;8(46):80826-80840. 9. Gu L, Ye P, Li H, et al. Lunasin attenuates oxidant-induced endothelial injury and inhibits atherosclerotic plaque progression in ApoE−/− mice by up-regulating heme oxygenase-1 via PI3K/Akt/Nrf2/ARE pathway[J]. The FASEB Journal. 2019 Apr;33(4):4836-4850. 10. Li X, Hu X, Tian G G, et al. C89 Induces Autophagy of Female Germline Stem Cells via Inhibition of the PI3K-Akt Pathway In Vitro[J]. Cells. 2019, 8(6): 606.

引用文献

1. Jiang Y, Zhao X, Chen J, et al.PM2. 5 induces cardiac malformations via PI3K/akt2/mTORC1 signaling pathway in zebrafish larvae.Environmental Pollution.2023: 121306. 2. Ye L, Huang Y, Liu X, et al.Apelin/APJ system protects placental trophoblasts from hypoxia-induced oxidative stress through activating PI3K/Akt signaling pathway in preeclampsia.Free Radical Biology and Medicine.2023 3. Zou X, Zeng M, Zheng Y, et al.Comparative Study of Hydroxytyrosol Acetate and Hydroxytyrosol in Activating Phase II Enzymes.Antioxidants.2023, 12(10): 1834. 4. Gao J, Wang N, Zong F, et al.TIPE2 regulates the response of BV2 cells to lipopolysaccharide by the crosstalk between PI3K/AKT signaling and microglia M1/M2 polarization.International Immunopharmacology.2023, 120: 110389. 5. Li W Y, Shi T S, Huang J, et al.Activation of the mTORC1 signaling cascade in the hippocampus and medial prefrontal cortex is required for the antidepressant actions of vortioxetine in mice.International Journal of Neuropsychopharmacology.2023: pyad017. 6. Shan X, Jiang R, Gou D, et al.Identification of a diketopiperazine‐based O‐GlcNAc transferase inhibitor sensitizing hepatocellular carcinoma to CDK9 inhibition.The FEBS Journal.2023 7. Tang P, Tang Y, Liu Y, et al.Quercetin-3-O-α-L-arabinopyranosyl-(1→ 2)-β-D-glucopyra-noside Isolated from Eucommia ulmoides Oliver Leaf Relieves Insulin Resistance in HepG2 cells via the IRS-1/PI3K/Akt/GSK-3β pathway.Biological and Pharmaceutical Bulletin.2022: b22-00597. 8. Zhang Z D, Li H X, Gan H, et al. RNF115 Inhibits the Post-ER Trafficking of TLRs and TLRs-Mediated Immune Responses by Catalyzing K11-Linked Ubiquitination of RAB1A and RAB13. Advanced Science. 2022: 2105391 9. Chen Y, Sun Y, Zhao W, et al. Elevated SRC3 expression predicts pemetrexed resistance in lung adenocarcinoma. Biomedicine & Pharmacotherapy. 2020, 125: 109958. 10. Gu L, Ye P, Li H, et al. Lunasin attenuates oxidant‐induced endothelial injury and inhibits atherosclerotic plaque progression in ApoE −/− mice by up‐regulating heme oxygenase‐1 via PI3K/Akt/Nrf2/ARE pathway. The FASEB Journal. 2019, 33(4): 4836-4850
11. Liu H, Liu Y, Wang H, et al. Geometric Constraints Regulate Energy Metabolism and Cellular Contractility in Vascular Smooth Muscle Cells by Coordinating Mitochondrial DNA Methylation. Advanced Science. 2022: 2203995. 12. Gu L, Wang Y, Xu Y, et al. Lunasin functionally enhances LDL uptake via inhibiting PCSK9 and enhancing LDLR expression in vitro and in vivo. Oncotarget. 2017 Aug 24;8(46):80826-80840 13. Xi H, Hu Z, Han S, et al. FSH-inhibited autophagy protects against oxidative stress in goat Sertoli cells through p62-Nrf2 pathway. Theriogenology. 2022 14. Pi Z, Lin H, Yang J. Isoflurane reduces pain and inhibits apoptosis of myocardial cells through the phosphoinositide 3-kinase/protein kinase B signaling pathway in mice during cardiac surgery. Molecular Medicine Reports. 2018 May;17(5):6497-6505 15. Wen Y, Peng D, Li C, et al. A new polysaccharide isolated from Morchella importuna fruiting bodies and its immunoregulatory mechanism. International Journal of Biological Macromolecules. 2019, 137: 8-19. 16. Li P, Lin Q, Sun S, et al. Inhibition of cannabinoid receptor type 1 sensitizes triple-negative breast cancer cells to ferroptosis via regulating fatty acid metabolism. Cell Death & Disease. 2022, 13(9): 1-15. 17. Du H, Wang R, Li J, et al. Ligustrazine induces viability, suppresses apoptosis and autophagy of retinal ganglion cells with ischemia/reperfusion injury through the PI3K/Akt/mTOR signaling pathway. Bioengineered. 2021, 12(1): 507-515. 18. Wang Y, Chen L, Lai S, et al. Connexin 43 contributes to the sensitization of colorectal cancer cells to photodynamic therapy through Akt inhibition. Photodiagnosis and Photodynamic Therapy. 2022: 103040. 19. Yizhuo L U, Lianghui L I, Guoyang W U, et al. Effect of PI3K/Akt Signaling Pathway on PRAS40Thr246 Phosphorylation in Gastric Cancer Cells. Iranian Journal of Public Health. 2019, 48(12): 2196-2204 20. Li X, Hu X, Tian G G, et al. C89 Induces Autophagy of Female Germline Stem Cells via Inhibition of the PI3K-Akt Pathway In Vitro. Cells. 2019, 8(6): 606 21. Sun Y, Wang L, Lu Q, et al. Phenols fragment of Veronica ciliata Fisch. Ameliorate free radical-induced nonalcoholic fatty liver disease by mediating PI3K/Akt signaling pathway. Journal of Ethnopharmacology. 2020: 112579. 22. Cen W J, Feng Y, Li S S, et al. Iron overload induces G1 phase arrest and autophagy in murine preosteoblast cells. Journal of cellular physiology. 2018, 233(9): 6779-6789. 23. Bai G, Wang H, Cui N. mTOR pathway mediates endoplasmic reticulum stress-induced CD4+ T cell apoptosis in septic mice. Apoptosis. 2022: 1-11 24. Chen Y, Sun Y, Zhao W, et al. Elevated SRC3 expression predicts pemetrexed resistance in lung adenocarcinoma. Biomedicine & Pharmacotherapy. 2020, 125: 109958. 25. Qiu W Q, Pan R, Tang Y, et al. Lychee seed polyphenol inhibits Aβ-induced activation of NLRP3 inflammasome via the LRP1/AMPK mediated autophagy induction. Biomedicine & Pharmacotherapy. 2020, 130: 110575. 26. Xiao H, Sun X, Lin Z, et al. Gentiopicroside targets PAQR3 to activate the PI3K/AKT signaling pathway and ameliorate disordered glucose and lipid metabolism. Acta Pharmaceutica Sinica B. 2022 27. Zhao Y, Guo W, Gu X, et al. Repression of deoxynivalenol-triggered cytotoxicity and apoptosis by mannan/β-glucans from yeast cell wall: Involvement of autophagy and PI3K-AKT-mTOR signaling pathway. International Journal of Biological Macromolecules. 2020, 164: 1413-1421 28. Wang J, Li Y, Wan C M, et al. PTEN inhibition leads to the development of resistance to novel isoquinoline derivative TNBG-5602 in human liver cancer cells. American Journal of Cancer Research. 2021, 11(9): 4515. 29. Cui L H, Li C X, Zhuo Y Z, et al. Saikosaponin d ameliorates pancreatic fibrosis by inhibiting autophagy of pancreatic stellate cells via PI3K/Akt/mTOR pathway. Chemico-biological interactions. 2019 Feb 25;300:18-26 30. Gu X, Guo W, Zhao Y, et al. Deoxynivalenol-Induced Cytotoxicity and Apoptosis in IPEC-J2 Cells Through the Activation of Autophagy by Inhibiting PI3K-AKT-mTOR Signaling Pathway. ACS Omega. 2019, 4(19): 18478-18486 31. Zhang H, Xia P, Liu J, et al. ATIC inhibits autophagy in hepatocellular cancer through the AKT/FOXO3 pathway and serves as a prognostic signature for modeling patient survival. International Journal of Biological Sciences. 2021, 17(15): 4442-4458. 32. Zhang W, Yang S, Chen D, et al. SOX2-OT induced by PAI-1 promotes triple-negative breast cancer cells metastasis by sponging miR-942-5p and activating PI3K/Akt signaling. Cellular and Molecular Life Sciences. 2022, 79(1): 1-16. 33. Li Y, Qu M, Xing F, et al. The Protective Mechanism of Dexmedetomidine in Regulating Atg14L-Beclin1-Vps34 Complex Against Myocardial Ischemia-Reperfusion Injury. Journal of Cardiovascular Translational Research. 2021 Dec;14(6):1063-1074. doi: 10.1007/s12265-021-10125-9. Epub 2021 Apr 29. 34. Xiao H, Sun X, Lin Z, et al. Gentiopicroside targets PAQR3 to activate PI3K/AKT signaling pathway and ameliorate glucose and lipid metabolism. Acta Pharmaceutica Sinica B. 2022 35. Lu J Y, Huang W T, Zhou K, et al. Microbial Lipopeptide Supramolecular Self‐Assemblies as a Methuosis‐Like Cell Death Inducer with In Vivo Antitumor Activity. Small. 2021: 2104034. 36. Liu Y, Wang J, Chen J, et al. Upregulation of miR-520c-3p via Hepatitis B Virus Drives Hepatocellular Migration and Invasion through the PTEN/AKT/NF-κB Signaling Pathway. Molecular Therapy-Nucleic Acids. 2022 37. Xie X, Zhang W, Zhou X, et al.Low doses of IFN-γ maintain self-renewal of leukemia stem cells in acute myeloid leukemia.Oncogene.2023: 1-13. 38. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12. 39. Chen F, Li X, Xiao Y, et al.Calcium phosphate ceramic-induced osteoimmunomodulation: Submicron-surface-treated macrophage-derived exosomes driving osteogenesis.Materials & Design.2024: 112903.
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投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください
投与量
mg/kg
動物の平均体重
g
動物あたりの投与量
ul
動物数
溶媒の組成を入力してください
% DMSO
%
% Tween 80
% ddH2O
計算する リセット

計算器

モル濃度計算機
希釈計算機
再構成計算
分子量計算機
=
X
X

モル度計算機では以下の計算が可能です

  • 既知の体積と濃度の溶液を調製するために必要な化合物の質量
  • 質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
  • 特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度
参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

X
=
X

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

=
/

バイアルを再構成するのに必要な溶媒の量を計算する.

再構成計算機を使えば、バイアルを再構成するための試薬の量をすぐに計算することができます.
試薬の質量と目標濃度を入力するだけで計算します。

g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

LY294002 154447-36-6 Apoptosis Autophagy DNA Damage/DNA Repair Metabolism PI3K/Akt/mTOR signaling Stem Cells DNA-PK Casein Kinase PI3K LY 294002 NSC-697286 Lysophosphatidic acid Leptin NPC NSC697286 NSC 697286 broad-spectrum Phosphoinositide 3-kinase DNA-dependent protein kinase CNE-2Z SF1101 reversibly Inhibitor inhibit YAP translocation LY-294002 carcinoma nasopharyngeal spermatozoa Human nuclear tumor SF 1101 SF-1101 inhibitor

 

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