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值分别为230nM、340nM、855nM、445nM、435nM、1100nM和290nM。
Cas No.:199596-05-9
Sample solution is provided at 25 µL, 10mM.
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JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 values of 230, 340, 855, 445, 435, 1100, and 290nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively[1]. Jumonji family histone demethylases, a class of enzymes that specifically remove methyl groups from histones, regulate gene expression and cellular functions, and play key roles in cell differentiation, development, gene silencing, and cancer progression[2]. JIB-04 is usually used in cancer and antiviral research[3][4].
In vitro, treatment of human aortic smooth muscle cells (HASMCs) with JIB-04 (0.5μM; 24-72h) inhibited cell proliferation and migration, arrested cell cycle at the G2/M phase, reduced cell viability, and decreased DNA replication[5]. JIB-04(0.25-1μM; 48-72h) inhibited cell viability and induced cell apoptosis of MHCC97H and HepG2 cells in a concentration-dependent manner[6].
In vivo, JIB-04 (50mg/kg; intratumoral injection; weekly for 3 weeks) reduced tumor volume and downregulated MECOM, EGR1, and KRAS expression in SKOV3 cell-derived ovarian cancer xenografts in SCID mice[7].
References:
[1] Wang L, Chang J, Varghese D, et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat Commun. 2013;4:2035.
[2] Park SY, Park JW, Chun YS. Jumonji histone demethylases as emerging therapeutic targets. Pharmacol Res. 2016;105:146-151.
[3] Lee J, Kim JS, Cho HI, Jo SR, Jang YK. JIB-04, a Pan-Inhibitor of Histone Demethylases, Targets Histone-Lysine-Demethylase-Dependent AKT Pathway, Leading to Cell Cycle Arrest and Inhibition of Cancer Stem-Like Cell Properties in Hepatocellular Carcinoma Cells. Int J Mol Sci. 2022;23(14):7657.
[4] Son J, Huang S, Zeng Q, et al. JIB-04 Has Broad-Spectrum Antiviral Activity and Inhibits SARS-CoV-2 Replication and Coronavirus Pathogenesis. mBio. 2022;13(1):e0337721.
[5] He Y, Yi X, Zhang Z, et al. JIB-04, a histone demethylase Jumonji C domain inhibitor, regulates phenotypic switching of vascular smooth muscle cells. Clin Epigenetics. 2022;14(1):101.
[6] Liao W, Liu J, Liu B, et al. JIB 04 induces cell apoptosis via activation of the p53/Bcl 2/caspase pathway in MHCC97H and HepG2 cells. Oncol Rep. 2018;40(6):3812-3820.
[7] Singh I, Karna A, Prajapati A, et al. Epigenetic targeting of MECOM/KRAS axis by JIB-04 impairs tumorigenesis and cisplatin resistance in MECOM-amplified ovarian cancer. Cell Death Discov. 2025;11(1):326.
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值分别为230nM、340nM、855nM、445nM、435nM、1100nM和290nM[1]。Jumonji家族组蛋白去甲基化酶是一类能够特异性去除组蛋白上甲基化修饰的酶，通过调节组蛋白的甲基化状态影响基因表达和细胞功能，在细胞分化、发育、基因沉默以及癌症发生等生物学过程中发挥着重要作用[2]。JIB-04常用于癌症和抗病毒研究[3][4]。
在体外实验中，用JIB-04（0.5μM；24-72小时）处理人主动脉平滑肌细胞（HASMCs）可以抑制细胞增殖和迁移，使细胞周期停滞在G2/M期，降低细胞活性，并减少DNA复制[5]。JIB-04（0.25-1μM；48-72小时）以浓度依赖的方式抑制MHCC97H和HepG2细胞的活性，并诱导细胞凋亡[6]。
在体内实验中，JIB-04（50mg/kg；瘤内注射；每周给药一次，持续3周）减少了SKOV3细胞来源的卵巢癌异种移植瘤在SCID小鼠中的肿瘤体积，并下调了MECOM、EGR1和KRAS的表达[7]。
| Cell experiment [1]: | |
Cell lines | human aortic smooth muscle cells |
Preparation Method | Human aortic smooth muscle cells (HASMCs) were separated from human ascending aortic tissue and cultured with DMEM/F12 with 10% fetal bovine serum and 1% penicillin-streptomycin. All cells were cultured at 37°C in a humidified incubator with 5% CO2. 4×103 cells/100μL per well were plated in 96-well plates and treated with DMSO or 0.5μM JIB-04 for 0h, 24h, 48h, or 72h. CCK-8 assay was performed to measure the toxicity of JIB-04 on HASMCs and the effect of JIB-04 on HASMC proliferation. A Cell-Light™ Edu Apollo 567 In Vitro kit was used to perform the EdU incorporation assay. |
Reaction Conditions | 0.5μM; 24-72h |
Applications | Treatment of human aortic smooth muscle cells (HASMCs) with JIB-04 inhibited cell proliferation, reduced cell viability, and decreased DNA replication. |
| Animal experiment [2]: | |
Animal models | female SCID mice |
Preparation Method | Female SCID mice were used in this experiment and were housed in specific-pathogen-free facilities with a 12h light/dark cycle and controlled temperature (20-22°C). Cell line-derived xenograft model was established as follows. Approximately 5×106 SKOV3 cells in 100μL DMEM medium were subcutaneously injected into the left flank of female SCID mice (6-8 weeks, n=6). Palpable tumors were observed about 20 days after induction. Tumor dimensions (mm) were measured using vernier calipers, and the volume of tumor was calculated using the formula V=length×(width)²×0.5. Mice were randomized by simple randomization into 2 groups, each comprising of 3 mice i.e., control group (DMSO as vehicle) and treatment group (50mg/kg JIB-04). Blinding was not implemented in this study. To minimize bias, standardized protocols were strictly followed. Additionally, two independent researchers verified the results to ensure objectivity. The mice were intratumorally injected weekly once with the drug for 3 weeks (0th, 7th, and 14th day). Tumor dimensions were measured on alternate days, and tumor volume was calculated and plotted as mean±SD. Statistical significance was measured using one-tailed paired t test considering p value<0.05 as statistically significant. Animals were sacrificed after 21 days of inhibitor administration. Tumors from both groups were excised and imaged. The tumor tissues were snap frozen in liquid nitrogen, and RNA was extracted to analyse target genes. |
Dosage form | 50mg/kg; intratumoral injection; weekly for 3 weeks |
Applications | JIB-04 reduced tumor volume and downregulated MECOM, EGR1, and KRAS expression in SKOV3 cell-derived ovarian cancer xenografts in SCID mice. |
References: | |
| Cas No. | 199596-05-9 | SDF | |
| 别名 | 5-氯-2(1H)-吡啶酮(2E)-(苯基-2-吡啶基亚甲基)腙 | ||
| 化学名 | 5-chloro-N-[(E)-[phenyl(pyridin-2-yl)methylidene]amino]pyridin-2-amine | ||
| Canonical SMILES | C1=CC=C(C=C1)C(=NNC2=NC=C(C=C2)Cl)C3=CC=CC=N3 | ||
| 分子式 | C17H13ClN4 | 分子量 | 308.76 |
| 溶解度 | ≥ 14.2mg/mL in DMSO | 储存条件 | Store at -20° C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2388 mL | 16.1938 mL | 32.3876 mL |
| 5 mM | 647.8 μL | 3.2388 mL | 6.4775 mL |
| 10 mM | 323.9 μL | 1.6194 mL | 3.2388 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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