| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
JIB-04 (also known as NSC693627) is a novel, potent and pan-selective inhibitor of Jumonji histone demethylase (JMJD) inhibitor with antineoplastic activity. As an epigenetic modifier, it inhibits JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D with IC50 values of 230, 340, 855, 445, 435, 1100, and 290 nM, respectively. JIB-04 inhibits cancer cell growth in vitro selectively and reduces in vivo tumor growth in H358 and A549 mouse xenograft models. It also prolongs the survival of mice with breast cancer.
| ln Vitro |
Compared to HBEC and PrSC/PrEC, JIB-04 was consistently more selective for cancer and normal cells, as demonstrated by its increased sensitivity in lung and prostate cancer cell lines (IC50 as low as 10nM). Jumonji demethylase activity in cells is inhibited by JIB-04, and JIB-04's function in cells is influenced by Jumonji levels [1]. The proliferation of GB cell lines and stem cell-enriched cultures is markedly inhibited by JIB-04. JIB-04 causes H3K4 hypermethylation, controls the expression of genes involved in limiting the proliferation of cancer cells, and has the strongest inhibitory effect on KDM5A. Furthermore, JIB-04 (2500 nM) inactivates PI3K and activates the pathways involved de autophagy and apoptosis. JIB-04 and TMZ work together to destroy GB cells as well[2].
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| ln Vivo |
JIB-04 significantly lowers the rates of cancer-related mortality in mice, extending their lifespan[1]. The mice's brains contain bioactive concentrations of JIB-04 (60, 40, and 20 mg/kg, ip). With a Hazard Ratio of 0.5, the orthotopic GB xenograft model indicates a tendency toward prolonged survival in mice treated with JIB-04[2].
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| Animal Protocol |
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| References |
| Molecular Formula |
C17H13CLN4
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| Molecular Weight |
308.76
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| Exact Mass |
308.082
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| CAS # |
199596-05-9
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| Related CAS # |
(Z)-JIB-04;199596-24-2
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| PubChem CID |
6519698
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
472.9±55.0 °C at 760 mmHg
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| Flash Point |
239.8±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.644
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| LogP |
3.92
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
368
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)/C(=N\NC2=NC=C(C=C2)Cl)/C3=CC=CC=N3
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| InChi Key |
YHHFKWKMXWRVTJ-OQKWZONESA-N
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| InChi Code |
InChI=1S/C17H13ClN4/c18-14-9-10-16(20-12-14)21-22-17(13-6-2-1-3-7-13)15-8-4-5-11-19-15/h1-12H,(H,20,21)/b22-17+
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| Chemical Name |
(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (4.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (32.39 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2388 mL | 16.1938 mL | 32.3876 mL | |
| 5 mM | 0.6478 mL | 3.2388 mL | 6.4775 mL | |
| 10 mM | 0.3239 mL | 1.6194 mL | 3.2388 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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