DASA-58 是有效的丙酮酸激酶 M2 (PKM2) 激活剂。DASA-58 可被用于代谢和多种癌症的研究。
| 生物活性 | DASA-58 is a potentialpyruvate kinaseisozyme (PKM2)allosteric activator. DASA-58 can be used for the research of metabolism and kinds ofcancer[1]. |
体外研究
(In Vitro) | DASA-58 (15 μM; 2 h) potentiates the antitumor effects of other metabolic stressors[1].
DASA-58 (15 μM; 24 h, 72 h) enhances pyruvate kinase activity in breast cancer cells without a clear effect on proliferation[1].
DASA-58 (30 μM, 60 μM; 0-72 h) enhances extracellular acidification and lactate levels in BCa cell lines and induce extracellular acidification levels in prostate cancer cell lines[1].
DASA-58 (15 μM, 30 μM; 0-72 h) affects respiration levels in BCa cells without an indication of mitochondrial damage[1].
DASA-58 (15 μM; 0-72 h) not rescues TXNIP levels in any combintion and mitochondrial inhibitors enhance PKM2 effects on activating AMPK signaling (T172 phosphorylation of AMPK)[1].
DASA-58 (15 μM; 0-72 h) leads to depletion in TXNIP levels independent of AMPK and ER signaling, and not through enhanced proteasomal degradation but rather depleted upstream glycolytic intermediates[1].
Cell Viability Assay[1] | Cell Line: | Five breast cancer cell lines (BCa cells)
(MDA MB 231, MDA MB 468, HCC 1443, T47-D, MCF7, LnCap, PC3, and DU145) | | Concentration: | 15 μM | | Incubation Time: | 2 h | | Result: | Could be exploited by other metabolic stressors. |
Western Blot Analysis[1] | Cell Line: | BCa cells | | Concentration: | 15 μM | | Incubation Time: | 24 h, 72 h | | Result: | Showed comparable PKM2 protein levels in five breast cancer cell lines, except HCC1443 cells and MDA MB 468 that showed the highest and lowest PKM2 protein levels, respectively.
Not changed PKM2 levels in five breast cancer cell lines but seemingly reduced TXNIP levels in cells expressing detectable TXNIP levels. |
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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 : ≥ 35 mg/mL(77.17 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.2049 mL | 11.0246 mL | 22.0493 mL | | 5 mM | 0.4410 mL | 2.2049 mL | 4.4099 mL | | 10 mM | 0.2205 mL | 1.1025 mL | 2.2049 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.59 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.59 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.59 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 20.8 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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