IOX1 | 5-羰基-8-羟基喹啉 | Histone Demethylase | 2OG Oxygenase

IOX1 化学结构
CAS号：5852-78-8

IOX1 3D分子结构
CAS号：5852-78-8

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IOX1 纯度/质量文件产品仅供科研

货号：A170634 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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IOX1 质控信息

产品名称	KDM1 ↓ ↑	KDM2 ↓ ↑	KDM3 ↓ ↑	KDM4 ↓ ↑	KDM5 ↓ ↑	KDM6 ↓ ↑	纯度
OG-L002	+++ LSD1, IC50: 20 nM						99%+
ORY-1001	+++ LSD1, IC50: 20 nM						98%
SP-2509	++++ LSD1, IC50: 13 nM						98+%
GSK2879552 2HCl	+ LSD1, Ki: 1.7 μM						99%+
T-3775440 HCl	++++ LSD1, IC50: 2.1 nM						99%
GSK-LSD1 2HCl	+++ LSD1, IC50: 16 nM						98%
Pulrodemstat benzenesulfonate	✔						99%+
IOX1		+ KDM2A, IC50: 1.8 μM	+++ KDM3A, IC50: 0.1 μM	++ KDM4E, IC50: 2.3 μM KDM4C, IC50: 0.6 μM	+ KDM5C, IC50: 19 μM	+ KDM6B, IC50: 1.6 μM	99%
PFI-90			✔				99%+
ML324				+ JMJD2, IC50: 920 nM			99%+
NCGC00244536				++++ KDM4, IC50: 10 nM			99%
KDM4D-IN-1				++ KDM4D, IC50: 0.41 μM			99%+
GSK467					++++ KDM5B, Ki: 10 nM		99%
GSK-J1						+++ JMJD3, IC50: 60 nM	99%+
(Z)-JIB-04				++ JMJD2A, IC50: 1100 nM JMJD2E, IC50: 340 nM	++ JARID1A, IC50: 230 nM	++ JMJD3, IC50: 855 nM	97%
CPI-455					++++ KDM5A, IC50: 10 nM	++++ KDM5, IC50: 10 nM	98%
JIB-04				++ JMJD2D, IC50: 290 nM JMJD2E, IC50: 435 nM	++ JARID1A, IC50: 230 nM	++ JMJD3, IC50: 855 nM	98%
GSK-J4 HCl						+++ JMJD3, IC50: 60 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

IOX1 生物活性

IOX1 细胞实验

IOX1 动物实验

IOX1 动物研究

IOX1 参考文献

IOX1 实验方案

IOX1 技术信息

Cell Line AGS cells MFC cells Mouse keratinocytes Human keratinocytes CT26 cells HCT116 cells CT26 cells HEK293 cells ESCC cells ESCC cells Murine CD4+ T cells Human peripheral blood CD4+ T cells A549 H1299 H1975 HeLa	Concentration	Treated Time	Description	References
AGS cells	5 μM	48 h	IOX1 significantly increased the expression of IFN-stimulated genes (ISGs), such as CXCL10, ISG15 and IFNB1	Adv Sci (Weinh). 2024 Oct;11(40):e2309983.
MFC cells	5 μM	48 h	IOX1 significantly increased the expression of IFN-stimulated genes (ISGs), such as CXCL10, ISG15 and IFNB1	Adv Sci (Weinh). 2024 Oct;11(40):e2309983.
Mouse keratinocytes	200 µM	24 h	To study the effect of IOX-1 on IL-23A expression, results showed that IOX-1 significantly reduced IL-23A expression.	Nat Commun. 2018 Apr 12;9(1):1420.
Human keratinocytes	200 µM	24 h	To study the effect of IOX-1 on IL-23A expression, results showed that IOX-1 significantly reduced IL-23A expression.	Nat Commun. 2018 Apr 12;9(1):1420.
CT26 cells	5, 25, 50 μM	24 h	Inhibited P-gp expression and enhanced DOX cytotoxicity	Nat Commun. 2021 Apr 23;12(1):2425.
HCT116 cells	5, 25, 50 μM	24 h	Inhibited P-gp expression and enhanced DOX cytotoxicity	Nat Commun. 2021 Apr 23;12(1):2425.
CT26 cells	25 μM	4 h	Enhanced DOX-induced immunogenic cell death (ICD)	Nat Commun. 2021 Apr 23;12(1):2425.
HEK293 cells	100 μM	24 h	To evaluate the inhibitory effect of IOX1 on histone demethylation, results showed that IOX1 treatment significantly increased the levels of me3Lys and me2Lys.	Anal Chem. 2017 Jan 17;89(2):1299-1306.
ESCC cells	50 µM	24 h	IOX1 increased H3K9me2 levels and slightly altered H3K27me3 levels, while decreasing the protein expression of KDM3A and KDM6B.	Cell Death Dis. 2020 Dec 14;11(12):1068.
ESCC cells	20 µM		IOX1 decreased the survival fraction of all ESCC cells and increased sensitivity to radiotherapy.	Cell Death Dis. 2020 Dec 14;11(12):1068.
Murine CD4+ T cells	10 μM and 20 μM	72 h	To evaluate the effect of IOX1 on Th1 and Th17 cell differentiation, results showed that IOX1 significantly suppressed IL-17 expression but had less effect on IFN-γ expression	EBioMedicine. 2022 Dec;86:104333.
Human peripheral blood CD4+ T cells	25 μM and 100 μM	5 days	To evaluate the effect of IOX1 on human CD4+ T cell proliferation and differentiation, results showed that IOX1 dose-dependently suppressed IFN-γ and IL-17 expression	EBioMedicine. 2022 Dec;86:104333.
A549	40 μM	48 h	IOX1 significantly enhanced the radiosensitivity of A549 cells, significantly increasing γirradiation-induced apoptosis.	Cell Death Dis. 2023 Dec 12;14(12):817.
H1299	40 μM	48 h	IOX1 significantly enhanced the radiosensitivity of H1299 cells, significantly increasing γirradiation-induced apoptosis.	Cell Death Dis. 2023 Dec 12;14(12):817.
H1975	40 μM	48 h	IOX1 significantly enhanced the radiosensitivity of H1975 cells, significantly increasing γirradiation-induced apoptosis.	Cell Death Dis. 2023 Dec 12;14(12):817.
HeLa	40 μM	48 h	IOX1 significantly enhanced the radiosensitivity of HeLa cells, significantly increasing γirradiation-induced apoptosis.	Cell Death Dis. 2023 Dec 12;14(12):817.

Species Mice Mice BALB/c mice B10.RIII mice Nude mice	Animal Model Renal ischemia-reperfusion injury model Subcutaneous xenograft model in nude mice S.c. CT26 tumour model Experimental autoimmune uveoretinitis (EAU) model A549 xenograft model	Administration	Dosage	Frequency	Description	References
Mice	Renal ischemia-reperfusion injury model	Tail vein injection	10 mg/kg	Single administration before surgery	IOX1 alleviates renal ischemia-reperfusion injury by increasing m6A methylation and regulating the CCL28/Treg/inflammatory cell axis.	Nat Commun. 2023 Mar 1;14(1):1161
Mice	Subcutaneous xenograft model in nude mice	Intraperitoneal injection	12.5 mg/kg	Every 2 days, continued treatment	IOX1 significantly suppressed tumor growth, decreased tumor volume, and reduced tumor weight	Adv Sci (Weinh). 2024 Oct;11(40):e2309983.
BALB/c mice	S.c. CT26 tumour model	Intravenous injection	7.5 mg/kg	Every 2 days for 3 times	IPLD significantly inhibited tumour growth and induced immune memory	Nat Commun. 2021 Apr 23;12(1):2425.
B10.RIII mice	Experimental autoimmune uveoretinitis (EAU) model	Intraperitoneal injection	12.5 mg/kg	Twice daily, until peak disease (Day 14)	To evaluate the effect of IOX1 on Th17 cell migration and inflammation in the EAU model, results showed that IOX1 significantly reduced the migration of Th17 cells into the site of inflammation and tissue damage	EBioMedicine. 2022 Dec;86:104333.
Nude mice	A549 xenograft model	Injection	10 mg/kg	Once a day for 6 days	IOX1 significantly suppressed the growth of A549 tumors and enhanced the tumor's sensitivity to radiation.	Cell Death Dis. 2023 Dec 12;14(12):817.

CAS号	5852-78-8
分子式	C₁₀H₇NO₃
分子量	189.17
SMILES Code	O=C(C1=C2C=CC=NC2=C(O)C=C1)O
MDL No.	MFCD18417145

别名	5-羰基-8-羟基喹啉
运输	蓝冰
InChI Key	JGRPKOGHYBAVMW-UHFFFAOYSA-N
Pubchem ID	459617

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 12 mg/mL(63.44 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

靶点	KDM2 KDM2A, IC50:1.8 μM KDM4 KDM4E, IC50:2.3 μM KDM4C, IC50:0.6 μM KDM6 KDM6B, IC50:1.6 μM KDM5 KDM5C, IC50:19 μM KDM3 KDM3A, IC50:0.1 μM
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]

Dose	Mice: 2.5 mg/kg^[3] (i.p.)
Administration	i.p.

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

IOX1 {[allProObj[0].p_purity_real_show]}

IOX1 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

IOX1 质控信息

IOX1 生物活性

IOX1 细胞实验

IOX1 动物实验

IOX1 动物研究

IOX1 参考文献

IOX1 实验方案

IOX1 技术信息

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靶点

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KDM2	KDM2A, IC50:1.8 μM
KDM4	KDM4E, IC50:2.3 μM KDM4C, IC50:0.6 μM
KDM6	KDM6B, IC50:1.6 μM
KDM5	KDM5C, IC50:19 μM
KDM3	KDM3A, IC50:0.1 μM

IOX1 {[allProObj[0].p_purity_real_show]}

IOX1 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

IOX1 质控信息

IOX1 生物活性

IOX1 细胞实验

IOX1 动物实验

IOX1 动物研究

IOX1 参考文献

IOX1 实验方案

IOX1 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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IOX1 纯度/质量文件产品仅供科研