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JIB-04
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JIB-04图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
JIB-04 是一种泛选择性 Jumonji 组蛋白去甲基化酶抑制剂,对 JARID1A、JMJD2E、JMJD3、JMJD2A、JMJD2B、JMJD2C 和 JMJD2D 的 IC50 分别为 230、340、855、445、435、1100 和 290 nM。

Cell lines

Human lung cancer cell lines (LCa); HBECs, Prostate cancer (PCa); Primary prostate stromal (PrSC) and prostate epithelial cells (PrEC).

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

4 days

Applications

JIB-04 shows selectivity of cancer cells (lung and prostate cancer lines with IC50 as low as 10 nM) over normal cells (HBECs and PrSCs/PrEC)s. Furthermore, 0.1–2 μM JIB-04 E-isomer decreases the total H3K9me3 demethylase activity, suggesting that JIB-04 inhibits H3K9me3 demethylases in cells at concentrations similar to the in vitro inhibition of individual purified enzymes.

Animal models

H358 and A549 lung cancer mice xenografts

Dosage form

Administered 2–3x weekly by IP injection at 110 mg/kg in sesame oil (H358 xenografts); Gavage in Cremophor EL at 55 mg/kg (A549 xenografts).

Applications

By comparing with vehicle treated groups, JIB-04 significantly abrogates the rate of tumor growth. It also markedly decreases the final tumor weights without effecting overall body weight or general health. In addition, JIB-04 lowers Jumonji histone demethylase activity in tumors and prolongs cancer survival.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

JIB-04 is a small molecule inhibitor of Jumonji histone demethylase with IC50 values of [1].

JIB-04 is a pyridine hydrazone. It is a pan -selective inhibitor of Jumonji histone demethylases. In a sensitive ELISA assay, JIB-04 inhibits JARID1A, JMJD2A, JMJD2B, JMJD2C, JMJD2E and JMJD3 with IC50 values of 230nM, 445nM, 435nM, 1100nM, 340nM and 855nM, respectively. Among the JMJD2 (KDM4) subfamily, JMJD2D has highest sensitivity. JIB-04 inhibits Jumonji demethylases in a unique manner. It is found not to be a competitive inhibitor of α-ketoglutarate in the competition assay [1].

JIB-04 shows consistently selective for cancer cells over normal cells. It has efficacy in cultured lung and prostate cancer lines with IC50 values as low as 10nM. JIB-04 is also effective in controlling lung cancer growth in animals. It significantly suppresses tumor growth of H358 and A549 lung cancer cell xenografts in mice with IC50 values of 100nM and 250nM, respectively. Furthermore, the anti-proliferation activity of JIB-04 results in a reduction in cancer-induced death rates in mice [1].

References:
[1] Wang L, Chang J, Varghese D, Dellinger M, Kumar S, Best AM, Ruiz J, Bruick R, Pena-Llopis S, Xu J, Babinski DJ, Frantz DE, Brekken RA, Quinn AM, Simeonov A, Easmon J, Martinez ED. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat Commun. 2013;4:2035.