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JIB-04

表观遗传修饰剂;抑制Jumonji组蛋白去甲基化酶

产品号 #(选择产品)

产品号 #73212_C

表观遗传修饰剂;抑制Jumonji组蛋白去甲基化酶

总览

JIB-04是一种表观遗传修饰剂,是一种Jumonji组蛋白去甲基化酶的广谱选择性抑制剂。它于高纳摩尔范围,可抑制该家族多个成员,JARID1A, JMJD2E, JMJD2B, JMJD2A,JMJD3和JMJD2C的IC₅₀值分别为230,340,435,445,855和1100 nM。它对组蛋白去乙酰化酶没有活性,对含铁酶甲基胞嘧啶双加氧酶TET1和脯氨酸羟化酶的作用很小(Wang等人;Easmon等人)。

癌症研究
·抑制多种人类肿瘤细胞系的增殖(Easmon等人)。
·在体外对肺癌或前列腺癌细胞具有选择性毒性,而对相同类型的正常细胞或从同一患者分离的正常对照系无毒性(Wang等人)。
·在乳腺癌小鼠模型中减少肿瘤负荷并延长生存期(Wang等人)。

细胞类型
癌细胞及细胞系
 
种属
人,小鼠,非人灵长类,其它细胞系,大鼠
 
研究领域
癌症
 
CAS 编号
199596-05-9
 
化学式
C₁₇H₁₃ClN₄
 
纯度
≥ 95 %
 
通路
表观遗传学
 
靶点
Jumonji
 

产品说明书及文档

请在《产品说明书》中查找相关支持信息和使用说明,或浏览下方更多实验方案。

Document Type
Product Name
Catalog #
Lot #
Language
Product Name
JIB-04
Catalog #
73212
Lot #
All
Language
English
Document Type
Safety Data Sheet
Product Name
JIB-04
Catalog #
73212
Lot #
All
Language
English

相关材料与文献

技术资料 (2)

文献 (2)

A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth Wang L et al. Nature Communications 2013

Abstract

The pharmacological inhibition of general transcriptional regulators has the potential to block growth through targeting multiple tumorigenic signalling pathways simultaneously. Here, using an innovative cell-based screen, we identify a structurally unique small molecule (named JIB-04) that specifically inhibits the activity of the Jumonji family of histone demethylases in vitro, in cancer cells, and in tumours in vivo. Unlike known inhibitors, JIB-04 is not a competitive inhibitor of α-ketoglutarate. In cancer, but not in patient-matched normal cells, JIB-04 alters a subset of transcriptional pathways and blocks viability. In mice, JIB-04 reduces tumour burden and prolongs survival. Importantly, we find that patients with breast tumours that overexpress Jumonji demethylases have significantly lower survival. Thus, JIB-04, a novel inhibitor of Jumonji demethylases in vitro and in vivo, constitutes a unique potential therapeutic and research tool against cancer, and validates the use of unbiased cellular screens to discover chemical modulators with disease relevance.
Azinyl and Diazinyl Hydrazones Derived from Aryl N -Heteroaryl Ketones: Synthesis and Antiproliferative Activity † , ‡ Easmon J et al. Journal of Medicinal Chemistry 1997

Abstract

A series of N-heteroaryl hydrazones derived from aryl N-heteroaryl or bis-N-heteroaryl methanones was prepared in search for potential novel antitumor agents. The stereochemistry of these compounds was established by means of NMR spectroscopy. Antiproliferative activity was determined in a panel of human tumor cell lines (CCRF-CEM, Burkitt's lymphoma, HeLa, ZR-75-1, HT-29, and MEXF 276L) in vitro. Generally, the new compounds were found to be more potent (IC50 = 0.011-0.436 microM) than the ribonucleotide reductase inhibitor hydroxyurea (IC50 = 140 microM). Most of the compounds exhibited the highest activity against Burkitt's lymphoma with an IC50 of 0.011-0.035 microM. [14C]Cytidine incorporation into DNA was quantitated for selected hydrazones (Z-A, E-1, Z-3, Z-4, E-5, Z-5, E-13, E-18, Z-19, Z-24, and E-26) as a measure of the inhibition of ribonucleotide reductase in Burkitt's lymphoma cells. The E-configurated compounds were found to inhibit [14C]cytidine incorporation to a greater extent (IC50 = 0.67-5.05 microM) than the Z-isomers (IC50 = 7.20 to textgreater 10 microM). Principal component analysis of the IC50 values obtained for inhibition of cell proliferation revealed that the cell lines tested can be grouped into three main families showing different sensitivities toward the compounds in our series [(i) CCRF-CEM, Burkitt's lymphoma, and Hela; (ii) HT-29; and (iii) MEXF 276 L].

更多信息

更多信息
种属 Human, Mouse, Non-Human Primate, Other, Rat
Cas Number 199596-05-9
Chemical Formula C₁₇H₁₃ClN₄
纯度 ≥ 95%
Target Jumonji
Pathway Epigenetic
质量保证:

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