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Submit ReviewIOX 1 is a histone demethylase JMJD inhibitor (IC50 values are 0.12, 0.17, 0.2, 0.3, 0.6 and 1 μM for JMJD3, JMJD1A, JMJD2A, JMJD2E, JMJD2C and UTX respectively). Cell permeable; it inhibits JMJD2A-mediated H3K9me3 demethylation in HeLa cells. IOX 1 suppresses IL-17 expression in mouse and human CD4+ T cells by targeting TET2. It also reduces infiltration of Th17 cells in an in vivo model of intraocular inflammation.
This compound is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the IOX 1 summary on the SGC website.
IOX 1 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 189.17 |
公式 | C10H7NO3 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 5852-78-8 |
PubChem ID | 459617 |
InChI Key | JGRPKOGHYBAVMW-UHFFFAOYSA-N |
Smiles | OC2=CC=C(C(O)=O)C1=CC=CN=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 18.92 | 100 | |
1eq. NaOH | 18.92 | 100 |
以下数据基于产品分子量 189.17。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 5.29 mL | 26.43 mL | 52.86 mL |
5 mM | 1.06 mL | 5.29 mL | 10.57 mL |
10 mM | 0.53 mL | 2.64 mL | 5.29 mL |
50 mM | 0.11 mL | 0.53 mL | 1.06 mL |
参考文献是支持产品生物活性的出版物。
King et al (2010) Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors. PLoS One. 5 e15535 PMID: 21124847
Hu et al (2022) Epigenetic drug screen identified IOX1 as an inhibitor of Th17-mediated inflammation through targeting TET2. EBioMedicine 86 104333 PMID: 36335665
If you know of a relevant reference for IOX 1, please let us know.
关键词: IOX 1, IOX 1 supplier, IOX1, histone, demethylases, inhibitors, inhibits, JMJD2, JMJD3, JMJD6, JMJD1, UTX, H3K9me3, demethylation, demethylates, cell, permeable, in, vitro, activity, sgc, T, cells, anti-inflammatory, Th17, IL-17, 5-carboxy-8HQ, Histone, Demethylases, 4464, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 IOX 1 的部分引用包括:
Christopher J et al (2022) Pharmacologic Targeting of TFIIH Suppresses KRAS-Mutant Pancreatic Ductal Adenocarcinoma and Synergizes with TRAIL. Cancer Res 82 3375-3393 PMID: 35819261
Li et al (2018) Epigenetic control of IL-23 expression in keratinocytes is important for chronic skin inflammation. Nat Commun 9 1420 PMID: 29650963
Sandra et al (2021) A KDM4A-PAF1-mediated epigenomic network is essential for acute myeloid leukemia cell self-renewal and survival. Cell Death Dis 12 573 PMID: 34083515
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.