GSK J4 HCl

目录号:S7070 批次号:S707005

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化学数据

化学结构式 别名 储存条件
(自收到货起)
3年 / -20°C / 粉状
1年 / -80°C / 溶于溶剂
化学式

C24H27N5O2.HCl

分子量 453.96 CAS号 1797983-09-5
Solubility (25°C)* 体外 DMSO 90 mg/mL (198.25 mM)
Ethanol 90 mg/mL (198.25 mM)
Water 9.4 mg/mL (20.7 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

产品描述 GSK J4 HCl是一种细胞渗透性的GSK J1前体药物,是第一个选择性H3K27组蛋白去甲基化酶JMJD3和UTX抑制剂,无细胞试验中IC50为60 nM,抑制JMJ家族的去甲基化酶活性。
靶点
JMJD3 [1]
(Cell-free assay)
60 nM
体外研究

GSK J4 HCl是JMJD3选择性组蛋白去甲基化酶抑制剂GSK-J1的乙酯类衍生物,IC50值大于50 μM。GSK J4 HCl用于探测H3K27me3去甲基化造成的后果。GSK-J4作用于人类原代巨噬细胞,抑制脂多糖诱导的细胞因子的产生,包括致炎的肿瘤坏死因子(TNF)。此外,GSK-J4抑制脂多糖诱导的与TNF转录起始位点相关的H3K27me3损失,并抑制RNA聚合酶II的招募。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

客户使用selleck产品的实验数据

, Nat Med, 2015, 21(6):555-9.

, Front Mol Neurosci, 2017, doi: 10.3389/fnmol.2017.00051

数据来源于[Data independently produced by , , Cell Mol Immunol, 2018, doi:10.1038/s41423-018-0037-8]

数据来源于[Data independently produced by , , FASEB J, 2018, 32(7):4031-4042]

GSK J4 HCl在文献中得到引用

Loss of Kmt2c or Kmt2d drives brain metastasis via KDM6A-dependent upregulation of MMP3 [ Nat Cell Biol, 2024, 26(7):1165-1175] PubMed: 38926506
Evi1 governs Kdm6b-mediated histone demethylation to regulate the Laptm4b-driven mTOR pathway in hematopoietic progenitor cells [ J Clin Invest, 2024, 134(24)e173403] PubMed: 39680456
Targeting lysine demethylase 6B ameliorates ASXL1 truncation-mediated myeloid malignancies in preclinical models [ J Clin Invest, 2024, 134(1)e163964] PubMed: 37917239
Refractory testicular germ cell tumors are highly sensitive to the targeting of polycomb pathway demethylases KDM6A and KDM6B [ Cell Commun Signal, 2024, 22(1):528] PubMed: 39482699
Dual targeting of histone deacetylases and MYC as potential treatment strategy for H3-K27M pediatric gliomas [ Elife, 2024, 13RP96257] PubMed: 39093942
Prenatal dexamethasone exposure reduces osteoprogenitor proliferation in mice via histone modifications at the Mkp-1 gene locus [ Commun Biol, 2024, 7(1):1589] PubMed: 39609620
Targeting histone demethylases JMJD3 and UTX: selenium as a potential therapeutic agent for cervical cancer [ Clin Epigenetics, 2024, 16(1):51] PubMed: 38576048
miRNA-27a-3p is involved in the plasticity of differentiated hepatocytes [ Gene, 2024, 913:148387] PubMed: 38499211
Refractory testicular germ cell tumors are highly sensitive to the targeting of polycomb pathway demethylases KDM6A and KDM6B [ Res Sq, 2024, rs.3.rs-4986186] PubMed: 39483904
Hedgehog pathway orchestrates the interplay of histone modifications and tailors combination epigenetic therapies in breast cancer [ Acta Pharm Sin B, 2023, 13(6):2601-2612] PubMed: 37425067

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品,在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同,大多数建议储存在-20°C,抑制剂属于化学试剂,可在常温下运输储存两周左右。即使如此,我们保证产品的出货量将保持产品质量的条件下,一般都会放入冰袋。望阁下收到产品后,请按照产品数据表建议适当存储。

如果需要长期保存,请于零下二十度低温保存。禁止用于人体及治疗!

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