5-羰基-8-羟基喹啉

用途生物活性体外研究体内研究 5-羰基-8-羟基喹啉试剂级价格

5-羰基-8-羟基喹啉

CAS号:5852-78-8
英文名:5-Carboxy-8-hydroxyquinoline
中文名:5-羰基-8-羟基喹啉
CBNumber:CB02671446
分子式:C10H7NO3
分子量:189.17
MOL File:5852-78-8.mol

5-羰基-8-羟基喹啉化学性质

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: soluble10mg/mL, clear
酸度系数(pKa) :1.82±0.10(Predicted)
形态 :powder
颜色 :white to brown
稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
InChIKey :JGRPKOGHYBAVMW-UHFFFAOYSA-N

安全信息

危险品标志 :Xn
危险类别码 :22
WGK Germany :3
海关编码 :2933499090

5-羰基-8-羟基喹啉性质、用途与生产工艺

用途
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)。
生物活性 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。

体外研究

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.

体内研究

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.