LY294002 是一种广谱PI3K抑制剂,抑制PI3Kα,PI3Kδ和PI3Kβ的IC50分别为 0.5, 0.57, 0.97 μM。LY294002 也可抑制CK2的活性,IC50为 98 nM。LY294002 是一种竞争性DNA-PK抑制剂,可逆结合 DNA-PK 的激酶结构域,IC50为 1.4 μM。LY294002 是一种凋亡 (apoptosis) 激活剂。
生物活性 | LY294002 is a broad-spectrum inhibitor ofPI3KwithIC50s of 0.5, 0.57, and 0.97 μM forPI3Kα,PI3KδandPI3Kβ, respectively[1]. LY294002 also inhibitsCK2with anIC50of 98 nM[2]. LY294002 is a competitiveDNA-PKinhibitor that binds reversibly to the kinase domain ofDNA-PKwith anIC50of 1.4 μM. LY294002 is anapoptosisactivator[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) |
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体外研究 (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].
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. |
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体内研究 (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].
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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(162.69 mM;Need ultrasonic) Ethanol : 50 mg/mL(162.69 mM;Need ultrasonic) 配制储备液 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 0.5%CMC-Na/saline water Solubility: 15.71 mg/mL (51.12 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 5% DMSO 95% (20%SBE-β-CDin saline) Solubility: 2.87 mg/mL (9.34 mM); Suspended solution; Need ultrasonic 3. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution
此方案可获得 ≥ 2.25 mg/mL (7.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 4. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution
此方案可获得 ≥ 2.25 mg/mL (7.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 5. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution
此方案可获得 ≥ 2.25 mg/mL (7.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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