5-羰基-8-羟基喹啉

5-羰基-8-羟基喹啉

中文名称5-羰基-8-羟基喹啉
中文同义词8-羟基喹啉-5-羧酸;5-羰基-8-羟基喹啉
英文名称5-Carboxy-8-hydroxyquinoline
英文同义词5-Carboxy-8-hydroxyquinoline;8-hydroxy-5-Quinolinecarboxylic acid;IOX 1, >=98%;JMJD2 Inhibitor, 5-carboxy-8HQ;8-Hydroxyquinoline-5-carboxylic acid 95%;JMJD2 Inhibitor, 5-carboxy-8HQ - CAS 5852-78-8 - Calbiochem;CS-1524;IOX-1;IOX 1
CAS号5852-78-8
分子式C10H7NO3
分子量189.17
EINECS号
相关类别小分子抑制剂,天然产物;染料中间体;小分子;Inhibitors;Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals;123456
Mol文件5852-78-8.mol
结构式5-羰基-8-羟基喹啉 结构式

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。
InChIKeyJGRPKOGHYBAVMW-UHFFFAOYSA-N

5-羰基-8-羟基喹啉 用途与合成方法

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.

安全信息

危险品标志Xn
危险类别码22
WGK Germany3
海关编码2933499090

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-12304IOX11 mg340元
2024/01/25HY-123045-羰基-8-羟基喹啉
IOX1
5852-78-85mg750元

5-羰基-8-羟基喹啉 上下游产品信息

"5-羰基-8-羟基喹啉"相关产品信息
曲古柳菌素A 2-[[(2-羟基-1-萘基)亚甲基]氨基]-N-(1-苯基乙基)苯甲酰胺 N/A 4-苯基丁酸钠盐 4-羟基-2-甲基喹啉 6-羟基喹啉 醌氢醌 邻氯苯胺 补骨脂甲素 对苯二酚 BIX01294 EPZ-6438 N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸乙酯 SGC-CBP30 5-氯-2(1H)-吡啶酮(2E)-(苯基-2-吡啶基亚甲基)腙 RVX-208
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