5-羰基-8-羟基喹啉
5-羰基-8-羟基喹啉 性质
熔点 | 301 °C (decomp) |
---|---|
沸点 | 464.5±30.0 °C(Predicted) |
密度 | 1.480±0.06 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶10mg/mL,澄清 |
酸度系数(pKa) | 1.82±0.10(Predicted) |
形态 | 粉末 |
颜色 | 白色至棕色 |
稳定性 | 自购买之日起 1 年内保持稳定。 DMSO 中的溶液可在 -20° 下保存长达 3 个月。 |
InChIKey | JGRPKOGHYBAVMW-UHFFFAOYSA-N |
5-羰基-8-羟基喹啉 用途与合成方法
5-羰基-8-羟基喹啉可用于抑制组蛋白赖氨酸脱甲基酶4A(KDM4A)。
IOX1,是 2OG 氧合酶 (2OG oxygenases) 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。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. 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. IOX1 (50-200 µM; 2 hours) attenuates cyclin D1 and upregulates p21 mRNA levels in a concentration-dependent. IOX1 (50-200 µM; 2 hours) mediates cyclin D1 and p21 expression by regaining H3K9me3.
Cell Proliferation Assay
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
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
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
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. |
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.
Animal Model: | Six-week-old male BALB/c nude mice |
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. |
5-羰基-8-羟基喹啉 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | HY-12304 | 1 mg | 340 | ||
2024-11-08 | HY-12304 | 5-羰基-8-羟基喹啉 | 5852-78-8 | 5mg | 750 |