JIB-04
(Synonyms: 5-氯-2(1H)-吡啶酮(2E)-(苯基-2-吡啶基亚甲基)腙) 目录号 : GC15603
A pan Jumonji histone demethylase inhibitor
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). |
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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 | |
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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 | 0.6478 mL | 3.2388 mL | 6.4775 mL |
| 10 mM | 0.3239 mL | 1.6194 mL | 3.2388 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet