产品说明书

JIB-04

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Chemical Structure| 199596-05-9 同义名 : -
CAS号 : 199596-05-9
货号 : A228395
分子式 : C17H13ClN4
纯度 : 98%
分子量 : 308.765
MDL号 : MFCD26936344
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(161.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 2 mg/mL(6.48 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
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

生物活性
靶点

  • KDM4

    JMJD2D, IC50:290 nM

    JMJD2E, IC50:435 nM

  • KDM6

    JMJD3, IC50:855 nM

  • KDM5

    JARID1A, IC50:230 nM
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
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.19mL

3.24mL

1.62mL

32.39mL

6.48mL

3.24mL
参考文献

[1]Wang L, Chang J, Varghese D, Dellinger M, Kumar S, Best AM, Ruiz J, Bruick R, Peña-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