JIB-04 (Synonyms: JHDM Inhibitor VII, NSC 693627) |
| Catalog No.GC15603 |
JMJIB-04는 JARID1A, JMJD2E, JMJD3, JMJD2A, JM에 대해 IC50이 각각 230, 340, 855, 445, 435, 1100 및 290nM인 범선택적 Jumonji 히스톤 데메틸라제 억제제입니다.
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 small molecule inhibitor of Jumonji histone demethylase with IC50 values of [1].
JIB-04 is a pyridine hydrazone. It is a pan -selective inhibitor of Jumonji histone demethylases. In a sensitive ELISA assay, JIB-04 inhibits JARID1A, JMJD2A, JMJD2B, JMJD2C, JMJD2E and JMJD3 with IC50 values of 230nM, 445nM, 435nM, 1100nM, 340nM and 855nM, respectively. Among the JMJD2 (KDM4) subfamily, JMJD2D has highest sensitivity. JIB-04 inhibits Jumonji demethylases in a unique manner. It is found not to be a competitive inhibitor of α-ketoglutarate in the competition assay [1].
JIB-04 shows consistently selective for cancer cells over normal cells. It has efficacy in cultured lung and prostate cancer lines with IC50 values as low as 10nM. JIB-04 is also effective in controlling lung cancer growth in animals. It significantly suppresses tumor growth of H358 and A549 lung cancer cell xenografts in mice with IC50 values of 100nM and 250nM, respectively. Furthermore, the anti-proliferation activity of JIB-04 results in a reduction in cancer-induced death rates in mice [1].
References:
[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.
| Cell experiment [1]: | |
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Cell lines |
Human lung cancer cell lines (LCa); HBECs, Prostate cancer (PCa); Primary prostate stromal (PrSC) and prostate epithelial cells (PrEC). |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
4 days |
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Applications |
JIB-04 shows selectivity of cancer cells (lung and prostate cancer lines with IC50 as low as 10 nM) over normal cells (HBECs and PrSCs/PrEC)s. Furthermore, 0.1–2 μM JIB-04 E-isomer decreases the total H3K9me3 demethylase activity, suggesting that JIB-04 inhibits H3K9me3 demethylases in cells at concentrations similar to the in vitro inhibition of individual purified enzymes. |
| Animal experiment [1]: | |
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Animal models |
H358 and A549 lung cancer mice xenografts |
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Dosage form |
Administered 2–3x weekly by IP injection at 110 mg/kg in sesame oil (H358 xenografts); Gavage in Cremophor EL at 55 mg/kg (A549 xenografts). |
|
Applications |
By comparing with vehicle treated groups, JIB-04 significantly abrogates the rate of tumor growth. It also markedly decreases the final tumor weights without effecting overall body weight or general health. In addition, JIB-04 lowers Jumonji histone demethylase activity in tumors and prolongs cancer survival. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
| 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 | 0.6478 mL | 3.2388 mL | 6.4775 mL |
| 10 mM | 0.3239 mL | 1.6194 mL | 3.2388 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 ddH2O, 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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