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LY294002

产品编号 T2008 CAS 154447-36-6

别名: LY 294002, NSC 697286, SF 1101

LY294002 (SF 1101) 是一种 PI3K 的广谱抑制剂，抑制 PI3Kα、PI3Kδ 和 PI3Kβ (IC50=0.5/0.57/0.97 μM)。LY294002 也是 DNA-PK 抑制剂 (IC50=1.4 μM) 和 CK2 抑制剂 (IC50=98 nM)。LY294002 可以激活凋亡和自噬。

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LY294002, CAS 154447-36-6

规格	价格/CNY	货期
5 mg	￥ 531	现货
10 mg	￥ 789	现货
50 mg	￥ 1,860	现货
100 mg	￥ 2,570	现货
200 mg	￥ 3,523	现货
500 mg	￥ 6,390	现货
1 mL * 10 mM (in DMSO)	￥ 531	现货

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其他形式的 LY294002:

LY-294002 hydrochloride
现货
PI-828
现货

选择批次

纯度: 99.93%

纯度: 99.92%

纯度: 99.76%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	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.
靶点活性	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)
体外活性	方法：人胰腺癌细胞 AsPC-1、BxPC-3 和 PANC-1 用 LY294002 (5-45 µM) 处理 24 h，使用 MTT 方法检测细胞生长抑制情况。结果：LY294002 剂量依赖诱导 AsPC-1、BxPC-3 和 PANC-1 细胞生长，IC50 分别为 40 μM、5 μM 和 35 μM。[1] 方法：表达人胰岛素受体的中国仓鼠卵巢细胞 CHO-IR 用 LY294002 (5 µM) 处理 5 min，并用 Insulin (1 nM, 10 min) 刺激，使用 Western Blot 方法检测靶点蛋白表达水平。结果：LY294002 可阻断 CHO-I R细胞中胰岛素诱导的 PKB Ser473 磷酸化。[2] 方法：人鼻咽癌细胞 CNE-2Z 用 LY294002 (10-75 μmol/L) 处理 24-48 h，使用 Flow Cytometry 方法检测细胞凋亡情况。结果：LY294002 剂量依赖性诱导 CNE-2Z 细胞凋亡。[3]
体内活性	方法：为检测体内抗肿瘤活性，将 LY294002 (25 mg/kg，每周两次) 和 cisplatin (5 mg/kg，每周一次) 腹腔注射给携带人胰腺癌肿瘤 AsPC-1 的 BALB/C nu/nu 小鼠，持续三周。结果：对照组小鼠的肿瘤体积增加，而 cisplatin 或 LY294002 治疗组的肿瘤体积分别减少为 77% 和 70%。联合治疗组更有效，肿瘤体积的生长下降到对照组体积的 44%。[4] 方法：为研究 PI3K 的药物阻断是否能改善 LPS 诱导的小鼠急性肝损伤的发展，将 LY294002 (40 μM; 10 μL) 单次腹腔注射给 LPS 诱导的急性肝损伤 BALB/c 小鼠模型。结果：LPS 诱导的肝炎中，LY294002 治疗明显抑制了各种疾病相关促炎细胞因子的肝内合成，包括肿瘤坏死因子-α、IL-6、IL-1β 和 INF-γ。在 LPS 损伤的小鼠肝脏样本中，观察到 LY294002 显著抑制 IκB 磷酸化。因此，LY294002 可能通过抑制活化的 B 细胞依赖性信号通路的 IκB 核因子 κ 轻链增强子来保护肝脏免受 LPS 诱导的损伤。[5]
激酶实验	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].
细胞实验	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].
动物实验	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].

别名	LY 294002, NSC 697286, SF 1101
分子量	307.34
分子式	C19H17NO3
CAS No.	154447-36-6

存储

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

溶解度

Ethanol: 10 mg/mL(32.5 mM)

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

DMSO: 34 mg/mL (110.6 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	3.2537 mL	16.2686 mL	32.5373 mL	81.3431 mL
	5 mM	0.6507 mL	3.2537 mL	6.5075 mL	16.2686 mL
	10 mM	0.3254 mL	1.6269 mL	3.2537 mL	8.1343 mL
	20 mM	0.1627 mL	0.8134 mL	1.6269 mL	4.0672 mL
DMSO	50 mM	0.0651 mL	0.3254 mL	0.6507 mL	1.6269 mL
DMSO	100 mM	0.0325 mL	0.1627 mL	0.3254 mL	0.8134 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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配液浓度

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.

文献引用

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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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

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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LY294002

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溶液配制表

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参考文献

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