|(E)-5-氯-2-(2-(苯基(吡啶-2-基)亚甲基)肼基)吡啶|CsnPharm

CAS No.: 199596-05-9

(E)-5-Chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine Catalog No. CSN13708

Synonyms: NSC 693627;JHDM Inhibitor VII

JIB-04 is a selective inhibitor of jumonji histone demethylase with IC50s of 230/340/855/445/435/1100, and 290 nM for JARID1A/JMJD2E/JMJD3/JMJD2A/JMJD2B/JMJD2C, and JMJD2D, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JMJD2C

IC50:1100nM JMJD2D

IC50:290nM JMJD2E

IC50:340nM JMJD3

IC50:855nM KDM5A

IC50:230nM
描述The overexpression of the Jumonji family of histone demethylases is associated with significantly lower survival in patients with breast cancer. JIB-04 is a small molecule inhibitor of the Jumonji enzymes. The IC50 values of JIB-04 for Jarid1A, JMJD2A, JMJD2B, JMJD2C, JMJD2E, and JMJD3 were 230 ± 40, 445 ± 30, 435 ± 70, 1100 ± 200, 340 ± 50, and 855 ± 5nM, respectively. JIB-04 exhibits high selectivity for cancer cells versus normal cells. The IC50 values of JIB-04 for lung and prostate cancer cell lines were as low as 10nM. Specifically, the IC50 values of JIB-04 for H358 and A549 lung cancer cells were 100 and 250nM, respectively. In immune-competent BALB/c mice inoculated with H358 or A549 lung cancer cells, administration of JIB-04 (H358 xenografts: 110mg/kg, intraperitoneal injection; A549 xenografts: 55mg/kg, oral gavage) two to three times weekly significantly decreased final tumor weights without affecting overall body weight or general health. The H358 and of A549 tumors isolated from the mice treated with JIB-04 also showed reduced total H3K9me3 demethylase activity compared to those collected from the vehicle-treated group. JIB-04 treatment also significantly extended the survival of tumor-bearing mice (18% increase in life span).^[3]
作用机制JIB-04 is pyridine hydrazine that inhibits the activity of Jumonji demethylases without affecting other α-ketoglutarate dependent hydroxylases or histone modifying enzymes.^[3]

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2387 mL
- 16.1936 mL
- 32.3871 mL
- 5 mM
- 0.6477 mL
- 3.2387 mL
- 6.4774 mL
- 10 mM
- 0.3239 mL
- 1.6194 mL
- 3.2387 mL

技术信息

CAS号

199596-05-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H13ClN4

运输

蓝冰

分子量

308.76

别名

NSC 693627;JHDM Inhibitor VII

溶解度

DMSO	200.0 mg/mL (647.7 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	4 mg/mL	clear
PO	0.5% CMC-Na	50 mg/mL	suspension

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

靶点	Description	IC50
JMJD2C		IC50:1100nM
JMJD2D		IC50:290nM
JMJD2E		IC50:340nM
JMJD3		IC50:855nM
KDM5A		IC50:230nM

(E)-5-Chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine Catalog No. CSN13708

靶点选择性

请登录您的专属账户

确认信息