|8-羟基喹啉-5-羧酸|CsnPharm

CAS No.: 5852-78-8

8-羟基喹啉-5-羧酸 Catalog No. CSN12941

IOX1 is the broad-spectrum inhibitor of 2OG oxygenases and its IC50 for KDM4A/KDM3A and KDM4C/KDM6B/KDM2A/KDM4E are 0.6/0.1 μM and 0.6 μM/1.6 μM/1.8 μM/2.3 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 KDM3A

IC50:0.1μM JMJD2C

IC50:0.6μM JMJD3

IC50:1.6μM KDM2A

IC50:1.8μM JMJD2E

IC50:2.3μM
描述The Jumonji C domain (JmjC) demethylases belong to the superfamily of Fe^II and 2-oxoglutarate (2OG) oxygenases. IOX1 is a potent inhibitor against a broad-spectrum of 2OG oxygenases, including non-JmjC 2OG oxygenases, with in vitro IC50 values in the micromolar range. Treatment of HeLa cells with 300μM of IOX1 led to a dose-dependent increase in H3K9me3 fluorescence intensity compared to the DMSO-treated control group. The cellular EC₅₀ value of IOX1 in HeLa cells was 100μM. The amplified luminescent proximity homogeneous assay revealed that the IC50 value of IOX1 for the inhibition of H3K9me3 demethylation activity of isolated KDM4C was 0.6μM. The IC50 values of IOX1 for KDM4E, KDM2A, KDM3A, KDM5C, KDM6B, and PHD2 were 2.3, 1.8, 0.1, 19.0, 1.4, and 33.0μM, respectively.^[3] In immunocompetent C57BL/6 mice harboring B16F10 tumors with a volume of about 50 mm³, repetitive intraperitoneal administration of IOX1 (2.5mg/kg) every two days significantly attenuated melanoma expansion at 10 days after treatment.^[4]
作用机制IOX1 is a potent, broad-spectrum 2OG oxygenase inhibitor with low cell permeability due to its polar C-5 carboxyl group.^[3]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HCT116 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay, IC50=28.1 μM	26491978
human A549 cells	-	Cytotoxicity assay	48 h	Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=48.3 μM	26491978
human HeLa cells	-	Function assay	72 h	Induction of histone methylation in human HeLa cells assessed as H3K9me2 level after 72 hrs by immunofluorescence assay	24325601

动物研究
剂量
Mice: 2.5 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 2.5 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Hu Q, Chen J, et al. IOX1, a JMJD2A inhibitor, suppresses the proliferation and migration of vascular smooth muscle cells induced by angiotensin II by regulating the expression of cell cycle-related proteins. Int J Mol Med. 2016 Jan;37(1):189-96.
[2] Schiller R, Scozzafava G, et al. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71.
[3] Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh TL, Chan MC, Mott BT, McCullagh JS, Maloney DJ, Schofield CJ, Kawamura A. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem. 2014 Mar;9(3):566-71
[4] Yu Y, Schleich K, Yue B, Ji S, Lohneis P, Kemper K, Silvis MR, Qutob N, van Rooijen E, Werner-Klein M, Li L, Dhawan D, Meierjohann S, Reimann M, Elkahloun A, Treitschke S, Dörken B, Speck C, Mallette FA, Zon LI, Holmen SL, Peeper DS, Samuels Y, Schmitt CA, Lee S. Targeting the Senescence-Overriding Cooperative Activity of Structurally Unrelated H3K9 Demethylases in Melanoma. Cancer Cell. 2018 Feb 12;33(2):322-336.e8

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.2863 mL
- 26.4316 mL
- 52.8632 mL
- 5 mM
- 1.0573 mL
- 5.2863 mL
- 10.5726 mL
- 10 mM
- 0.5286 mL
- 2.6432 mL
- 5.2863 mL

技术信息

CAS号

5852-78-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H7NO3

运输

蓝冰

分子量

189.17

别名

溶解度

DMSO	37.0 mg/mL (195.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
KDM3A		IC50:0.1μM
JMJD2C		IC50:0.6μM
JMJD3		IC50:1.6μM
KDM2A		IC50:1.8μM
JMJD2E		IC50:2.3μM

8-羟基喹啉-5-羧酸 Catalog No. CSN12941

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