IOX1，是 2OG 氧合酶 (2OGoxygenases) 的有效广谱抑制剂，包括 JmjC 去甲基酶。IOX1 抑制 KDM4C，KDM4E，KDM2A，KDM3A 和 KDM6B 的IC50值分别为 0.6 μM，2.3 μM，1.8 μM，0.1 μM 和 1.4 μM。IOX1 抑制 ALKBH5。
| 生物活性 | IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of2OGoxygenases, including theJmjCdemethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B withIC50values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively[1][2]. IOX1 also inhibits ALKBH5[3]. |
体外研究
(In Vitro) | IOX1 (0-200 μM; 2 hours) inhibits the proliferation and migration of vascular smooth muscle cells (VSMCs) stimulated with angiotensin II (Ang II) in a concentration-dependent manner[2].IOX1 (200 μM; 24 hours) blocks the cell cycle progression of angiotensin II (Ang II)-VSMCs by increasing the percentage of cells in the G0/G1 phase[2].IOX1 (50-200 μM; 2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in a concentration-dependent[2].IOX1 (50-200 μM; 2 hours) mediates cyclin D1 and p21 expression by regaining H3K9me3[2].
Cell Proliferation Assay[2] | Cell Line: | Vascular smooth muscle cells (VSMCs) | | Concentration: | 50 μM, 100 μM, 200 μM | | Incubation Time: | Pretreated 2 hours | | Result: | Exhibited a decrease in proliferation and migration. |
Cell Cycle Analysis[2] | Cell Line: | Vascular smooth muscle cells (VSMCs) | | Concentration: | 200 μM | | Incubation Time: | 24 hours | | Result: | Slowed down the progression of the cell cycle from the G0/G1 to the S phase. |
RT-PCR[2] | Cell Line: | Vascular smooth muscle cells (VSMCs) | | Concentration: | 50 μM, 100 μM, 200 μM | | Incubation Time: | 2 hours | | Result: | Decreased cyclin D1 mRNA expression and increased p21 mRNA expression. |
RT-PCR[2] | Cell Line: | Vascular smooth muscle cells (VSMCs) | | Concentration: | 50 μM, 100 μM, 200 μM | | Incubation Time: | 2 hours | | Result: | Enhanced the total protein levels of H3K9me3. |
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体内研究
(In Vivo) | IOX1 (5-c-8HQ) (oral gavage; 10-20 mg/kg; 12 days) inhibits tumor growth and attenuates the self-renewal of liver cancer stem-like cells (LCSCs) in vivo[1].
| Animal Model: | Six-week-old male BALB/c nude mice[4] | | Dosage: | 10 mg/kg, 20 mg/kg | | Administration: | 12 days | | Result: | Did not result in obvious adverse effects on mice as demonstrated by no body weight reduction and no toxicity to the major organs after treatment.Inhibited LCSC orthotopic graft tumor growth.Significantly reduced the protein levels of EpCAM and Sox9 in LCSC orthotopic graft tumors nhibited LCSC orthotopic graft tumor growth.Decreased Ki67-positive tumor cells and markedly reduced the tumorsphere formation abilities of LCSCs 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 : 13.33 mg/mL(70.47 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 5.2863 mL | 26.4313 mL | 52.8625 mL | | 5 mM | 1.0573 mL | 5.2863 mL | 10.5725 mL | | 10 mM | 0.5286 mL | 2.6431 mL | 5.2863 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 (11.00 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (11.00 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 (11.00 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (11.00 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。 *以上所有助溶剂都可在本网站选购。
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