LY294002
目录号：S1105 别名： SF 1101, NSC 697286
Molecular Weight(MW): 307.34
LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。
客户使用该产品的15个实验数据：
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Type I IFNs induce ISG expression in a serine phosphorylation-independent manner. Cells were treated with kinase inhibitors (SB203580, rottlerin, Ly294002, PD98059, and SP600125) before stimulation with IFN-a and IFN-b for 6 hours. Cell lysates were used in western blotting and probed for serine phosphorylation.The relative amounts of pSTAT1 S727 in (up-graph) were quantied and normalized to an untreated control (below-graph).
Hepatology 2014 59(4), 1262-72. LY294002 purchased from Selleck.
different signal-inhibitory profile by applying 120 nmol/L BGT226, 20 μmol/L LY294002, or 100 nmol/L rapamycin in FaDu cells.
Clin Cancer Res 2011 17, 7116-7126. LY294002 purchased from Selleck.
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Stimulation response of p37d-expressing cells. (c) Western blot of 5 min serum stimulated HEK-293 cells stably expressing p37d, p110d or control, with the presence of inhibitors as indicated at the top.
Oncogene 2012 31, 3277–3286. LY294002 purchased from Selleck.
Immunofluorescence and flow cytometric analyses of the translocation of ABCG2 in MCF-7 FLV1000 cells before and after treatment with the PI3K inhibitor LY294002. Confocal microscopy of MCF-7 FLV1000 cells after a 16-h treatment with 2 uM or 4 uM of LY294002 was performed as described in Figure.
Br J Pharmacol 2013 70(5), 1137-51. LY294002 purchased from Selleck.
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SCC61 or Detroit 562 xenografted tumors respond to treatment by PI3K inhibitor, LY294002 alone, or in combination with gefitinib. % tumor growth is shown. By two-way ANOVA, the effect of treatment and time is considered significant;
Mol Oncol 2013 7, 359-68. LY294002 purchased from Selleck.
Inhibition of EGFR and PI3K/AKT pathway has additive effects in SCCHN cell lines with constitutively active PIK3CA mutations, while removing negative regulation of PI3K/AKT pathway increases resistance in sensitive SCCHN cell line. A, results from MTT assays on cells treated with PI3K inhibitor, LY294002, and gefitinib.
Mol Oncol 2013 7, 359-68. LY294002 purchased from Selleck.
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Lyn-PI3K-BTK signaling is required for the inhibitory effect of anti-CD180 on the activation of IFN-α signaling. (a and b) Isolated murine splenic B220+ B cells were pretreated with dasatinib (5 μM), a Lyn inhibitor; LY294002 (5 μM), a PI3K inhibitor; ibturinib (1 μM), a BTK inhibitor; enzastaurin (1 μM), a PKC β inhibitor; U0126 (3 μM), an ERK inhibitor; SP600126 (2 μM), a JNK inhibitor or SB20358 (1 μM), a p38 inhibitor for 1 h, followed by stimulation with anti-CD180 antibody (0.2 μg/mL) or mouse IFN-α (1000 U/mL) for 4 h. qPCR analysis of the expression of IFIT1 (a) and MX1 (b). (c) Isolated murine splenic B220+ B cells were pretreated with dasatinib (5 μM), LY294002 (5 μM), and ibturinib (1 μM) for 1 h, followed by stimulation with anti-CD180 antibody (0.2 μg mL−1) or mouse IFN-α (1000 U mL−1) for 40 min. Western blot analysis of the phosphorylation level of STAT-2. The data shown represent the mean values of three independent experiments, and the error bars represent the SEM. *p < 0.05, **p < 0.01, ***p < 0.001, as determined by ANOVA; ns denotes p > 0.05.
Cell Mol Immunol, 2017, 14(2):192-202. LY294002 purchased from Selleck.
The effects of GLP-1R siRNA and LY294002 on neurological score at 24 hours after subarachnoid hemorrhage (SAH) in Ex-4 treated rats.
Neuropharmacology, 2018, 128:142-151. LY294002 purchased from Selleck.
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Comparative effects of inhibitors by immunofluorescence microscopy study. Confluent HC11 cells were grown on poly-L-lysine-coated glass coverslips (immunofluorescence) and on plastic plates (biochemical control) and then treated with inhibitors according to the standard procedure. Upper part: the biochemical action of the inhibitors was tested to validate the immunofluorescence results. Cellular proteins were analyzed by SDS-PAGE and the immunoblots were successively probed with anti-ADRP, anti-β-casein, and anti- β-actin antibodies and their respective HRP-conjugated secondary antibodies. Each experimental condition was performed in duplicate. Lower part: cells were fixed, permeabilized and subjected to immunofluorescence microscopy using antiserum against ADRP and TRITC-conjugated secondary antibody (red).
Biochim Biophys Acta 2012 1823(5), 987-96. LY294002 purchased from Selleck.
Comparative effects of wortmannin and LY294002 on ADRP and β -casein synthesis. Con fluent HC11 cells were treated according to the standard procedure in the absence or presence of 4 ng/ml EGF either with or without 100 nM wortmannin or 50μM LY294002. Cellular proteins were analyzed by SDS-PAGE and immunoblot successively probed with anti-ADRP, anti-β-casein, anti-β -actin antibodies and their respective HRP-conjugated secondary antibodies. ECL signals were quantified by densitometry and normalized to β-actin. Each experimental condition was performed in triplicate. Percentages of inhibition for both inhibitor and hormonal treatments are indicated in the text.
Biochim Biophys Acta 2012 1823(5), 987-96. LY294002 purchased from Selleck.
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Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.
Int J Biochem Cell Biol 2015 60, 34-42. LY294002 purchased from Selleck.
IGF1 increases apical fibronectin in late stage blastocysts. Representative confocal images of blastocysts stained for fibronectin (Green) and DAPI (Blue). Day 5 blastocysts were cultured in SS medium for 24 (A and B), 48 (C and D) or 72 h (E-H) in the absence (A, C and E) or presence (B, D and F) of 10 ng/ml IGF1 or in the presence of a PI3 Kinase inhibitor (5 uM LY294002 + 10 ng/ml IGF1) (G) or in the presence of 10 ng/ml IGF1, attached to a coverslip (H). Scale bars represent 20 mm. Red line indicates location of coverslip. Arrow indicates location of the inner cell mass (ICM). The following total number of blastocysts were analysed, from at least 3 experimental repeats in each treatment; 24 in the SS group (24 h), 21 in SS plus IGF1 (24 h), 26 in SS (48 h), 30 in SS plus IGF1 (48 h), 40 in SS (72 h), 59 in SS plus IGF1 (72 h), 13 in SS plus IGF1 + LY294002 (48 h) and 15 blastocysts were analysed that were attached to a coverslip (72 h).
Hum Reprod 2015 30(2), 284-98. LY294002 purchased from Selleck.
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PTEN transfection or inhibition of the PI3K-AKT and IGF-1R signaling pathways increases the trastuzumab sensitivity of NCI-N87/TR cells. After treating the cells with a PI3K inhibitor (LY294002), the expression of AKT and P-AKT proteins was assessed by Western blotting. Tubulin expression indicated equal loading. All gels run under the same experimental conditions and the experiments were repeated 3 times. The representative images were cropped and shown. Control: cells without any treatment.
Sci Rep 2015 5, 11634. LY294002 purchased from Selleck.
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
2010 Saraswati Sukumar of Johns Hopkins University School of Medicine. LY294002 purchased from Selleck.
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T47Dcells were pretreated with 100 ng/ml EGF for 20 min and then treated with the indicated concentrations of LY294002 for 24 hours.
2010 Dr. Zhang of Tianjin Medical University. LY294002 purchased from Selleck.
产品安全说明书
PI3K抑制剂选择性比较
生物活性
| 产品描述 | LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 特性 | LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 靶点 |
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| 体外研究 |
LY294002是一种非特异性抑制剂，除了class I PI3Ks，它同样还能抑制其他类型PI3Ks、mTOR、DNA-PK以及其他蛋白激酶，如CK2和Pim-1[5]。LY294002使Akt/PKB失活,因此抑制细胞增殖和诱导细胞凋亡。 LY294002作用于结肠癌细胞系，使磷酸化Akt (Ser473)的表达下降， 明显抑制生长和诱导凋亡。[2] LY294002作用于肿瘤细胞，诱导明显的核固缩和减少细胞质体积。因此，在体外，LY294002明显抑制卵巢癌细胞增殖。LY294002诱导细胞停在G1期，导致几乎全部的黑色素瘤细胞增殖被抑制，部分MG-63 (骨肉瘤细胞系)增殖被抑制。LY294002作用于细胞周期的效果可用于研究PI3K激活通路和癌细胞周期之间关系。[3] |
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| Cell Data |
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| 体内研究 | 体内，LY294002也抑制肿瘤生长和诱导凋亡，尤其作用于LoVo肿瘤, 因此作用于鼠癌性腹膜炎模型具有明显药效。[2] LY294002明显抑制卵巢癌生长和腹水形成。[3] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验： |
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激酶实验: 使用重组酶和1 μM ATP，通过辐射实验测定LY294002对PI3K的抑制效果。室温下(24oC)进行激酶反应1小时，然后加入PBS终止反应。通过剂量反应曲线测定IC50值。通过激酶选择性筛选来抑制CK2和GSK3β。加入10 μM ATP，测定LY294002作用于一组激酶的效果。 |
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| 细胞实验： |
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| 动物实验： |
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溶解度 (25°C)
| 体外 | DMSO | 36 mg/mL (117.13 mM) |
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| Ethanol | 21 mg/mL (68.32 mM) | |
| Water | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 4% DMSO+30% PEG 300+5% Tween 80+ddH2O |
5mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 307.34 |
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| 化学式 | C19H17NO3 |
| CAS号 | 154447-36-6 |
| 稳定性 | powder |
| in solvent | |
| 别名 | SF 1101, NSC 697286 |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
技术支持
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常见问题及建议解决方法
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问题 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?
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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.
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问题 2：
What is the suggested formulation of this compound for mouse injection(i.p.)?
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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.
