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5852-78-8

中文名稱 5-羰基-8-羥基喹啉
英文名稱 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 2024/12/18 11:16:59
5852-78-8 結(jié)構(gòu)式 5852-78-8 結(jié)構(gòu)式

基本信息

中文別名
5-羰基-8-羥基喹啉
8-羥基喹啉-5-羧酸
英文別名
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
所屬類別
生物化工:Histone Demethylase 抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)301 °C (decomp)
沸點(diǎn)464.5±30.0 °C(Predicted)
密度1.480±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO:可溶10mg/mL,澄清
酸度系數(shù)(pKa)1.82±0.10(Predicted)
形態(tài)粉末
顏色白色至棕色
穩(wěn)定性自購買之日起 1 年內(nèi)保持穩(wěn)定。 DMSO 中的溶液可在 -20° 下保存長達(dá) 3 個(gè)月。
InChIKeyJGRPKOGHYBAVMW-UHFFFAOYSA-N

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302
防范說明P261-P271-P280
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類別碼22
WGK Germany3
海關(guān)編碼2933499090

常見問題列表

用途

5-羰基-8-羥基喹啉可用于抑制組蛋白賴氨酸脫甲基酶4A(KDM4A)。

生物活性
IOX1,是 2OG 氧合酶 (2OG oxygenases) 的有效廣譜抑制劑,包括 JmjC 去甲基酶。IOX1 抑制 KDM4C,KDM4E,KDM2A,KDM3A 和 KDM6B 的 IC50 值分別為 0.6 μM,2.3 μM,1.8 μM,0.1 μM 和 1.4 μM。IOX1 抑制 ALKBH5。
體外研究

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.
體內(nèi)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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