Meisoindigo (Dian III) 是 Indirubin (HY-N0117) 的衍生物，可以造成急性髓细胞性白血病 (AML) 细胞周期在 G0/G1 期停滞，并诱导凋亡。Meisoindigo 具有很高的抗肿瘤活性。
| 生物活性 | Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and inducesapoptosisin primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity[1][2]. |
体外研究
(In Vitro) | Meisoindigo (Dian III; 5-20 μM; for 24 hours) inhibits growth of the AML cell lines[1].
Meisoindigo (10 μM; for 24 hours) induces apoptosis of acute myeloid leukemia[1].
Meisoindigo (5-10 μM; for 24 hours) causes cell-cycle arrest[1].
Meisoindigo (5-10 μM; for 24 hours) increases the cleaved caspase-3 and pro-apoptotic Bak, and decreases Bcl-2 and Bcl-xL levels in HL-60 cells[1].
Meisoindigo (10, 30, 50, 100, 150 μM; 24 hours) interdicts LPS-induced (1 μg/mL) NLRP3 inflammasome activation and M1/M2 polarization through down-regulation of TLR4 pathways after OGD/R in HT-22 and BV2 cells[2].
Cell Viability Assay[1] | Cell Line: | HL-60, NB4, U937 leukemic cell lines | | Concentration: | 5, 10, 15, 20 μM | | Incubation Time: | For 24 hours | | Result: | Inhibited growth of the AML cell lines in a dose- and time-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | HL-60 cells | | Concentration: | 10 μM | | Incubation Time: | For 24 hours | | Result: | Induced apoptosis of acute myeloid leukemia. |
Cell Cycle Analysis[1] | Cell Line: | HL-60 cells | | Concentration: | 5, 10 μM | | Incubation Time: | For 24 hours | | Result: | Caused cell-cycle arrest, with more cells in sub-G1 and G0/G1 phases and fewer cells in the S phase, in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | HL-60 cells | | Concentration: | 5, 10 μM | | Incubation Time: | For 24 hours | | Result: | Increased the cleaved caspase-3 and pro-apoptotic Bak, and decreased Bcl-2 and Bcl-xL levels in HL-60 cells. |
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体内研究
(In Vivo) | Meisoindigo (Dian III; 50-150 mg/kg; IP; daily; for 14 days) has anti-leukemic activity in vivo[1].
Meisoindigo (2, 4, 8, 12 mg/kg; IP; before MCAO and 2 h after reperfusion) significantly reduces infarct volume, ameliorates neurological deficits 3 days after middle cerebral artery occlusion (MCAO) in Wild-type C57BL/6J mice (25-30 g). Meisoindigo reduces edema and lowers AQP4 expression in the brain[2].
| Animal Model: | NOD/SCID mice, 6-8 weeks old, with HL-60 leukemic cells[1] | | Dosage: | 50, 100, 150 mg/kg | | Administration: | IP; daily; for 14 days | | Result: | Had anti-leukemic activity in vivo. |
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| 结构分类 | - Alkaloids
- Indole Alkaloids
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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 : ≥ 51 mg/mL(184.59 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.6194 mL | 18.0969 mL | 36.1939 mL | | 5 mM | 0.7239 mL | 3.6194 mL | 7.2388 mL | | 10 mM | 0.3619 mL | 1.8097 mL | 3.6194 mL |
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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: ≥ 2.5 mg/mL (9.05 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.05 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 *以上所有助溶剂都可在本网站选购。
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