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5852-78-8

中文名称 5-羰基-8-羟基喹啉
英文名称 5-Carboxy-8-hydroxyquinoline
CAS 5852-78-8
分子式 C10H7NO3
分子量 189.17
MOL 文件 5852-78-8.mol
更新日期 2024/05/20 09:19:54
5852-78-8 结构式 5852-78-8 结构式

基本信息

中文别名
5-羰基-8-羟基喹啉
8-羟基喹啉-5-羧酸
英文别名
IOX1
CS-1524
IOX-1
IOX 1
IOX 1, >=98%
5-Carboxy-8-hydroxyquinoline
JMJD2 Inhibitor, 5-carboxy-8HQ
8-hydroxy-5-Quinolinecarboxylic acid
8-Hydroxyquinoline-5-carboxylic Acid
5-Quinolinecarboxylic acid, 8-hydroxy-
5-Carboxy-8-hydroxyquinoline USP/EP/BP
所属类别
生物化工:Histone Demethylase 抑制剂

物理化学性质

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: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。
InChIKeyJGRPKOGHYBAVMW-UHFFFAOYSA-N

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
防范说明P261-P271-P280
危险品标志Xn
危险类别码22
WGK Germany3
海关编码2933499090

常见问题列表

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.
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