JIB-04 (Synonyms: JHDM Inhibitor VII, NSC 693627) |
Catalog No.GC15603
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Synonyms | JHDM Inhibitor VII, NSC 693627 | ||
| Chemical Name | 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 | ||
| Formula | C17H13ClN4 | M.Wt | 308.76 |
| Solubility | ≥ 14.2mg/mL in DMSO | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)