JIB-04|199596-05-9|-陌孚医药/Medlife

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JIB-04

目录号: PL15128 纯度: ≥98%

CAS No. :199596-05-9

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中文名称	JIB-04
中文别名	5-氯-2(1H)-吡啶酮 (2E)-(苯基-2-吡啶基亚甲基)腙;JIB-04(NSC 693627) 抑制剂;5-氯-N[[(E)- [苯基(吡啶-2-基)甲叉基]氨基]吡啶-2-胺
英文名称	JIB-04
英文别名	5-chloro-N-[(E)-[phenyl(pyridin-2-yl)methylidene]amino]pyridin-2-amine;AC1O75RE;FD5031;NSC-693627;JIB-04, NSC 693627;QC-10233;S7281,NSC693627,;JIB-04;(E)-N-(5-Chloro-pyridin-2-yl)?-N-(phenyl-pyridin-2-yl-methylene)-hydrazine;JIB 04;JIB-04 (NSC 693627)(E);(E)-5-CHLORO-2-(2-(PHENYL(PYRIDIN-2-YL)METHYLENE)HYDRAZINYL)PYRIDINE;(E)-N-(5-Chloro-pyridin-2-yl)-N′-(phenyl-pyridin-2-yl-methylene)-hydrazine;NSC 693627;JIB-04 (E);NSC693627 (E);JIB-04 (NSC 693627);5-Chloro-2(1H)-pyridinone (2E)-(phenyl-2-pyridinylmethylene)hydrazone;JIB04;NCIChal_000041;5-Chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine;AK314648;NCI60_033523
Cas No.	199596-05-9
分子式	C₁₇H₁₃ClN₄
分子量	308.76
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	JIB-04 是 Jumonji 组蛋白去甲基酶 (Jumonji histone demethylase) 广谱抑制剂，能抑制 JARID1A，JMJD2E，JMJD3，JMJD2A，JMJD2B，JMJD2C 和 JMJD2D 的活性，其 IC₅₀ 值分别为 230，340，855，445，435，1100 和 290 nM。
生物活性	JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC 50 s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 230 nM (JARID1A), 445 nM (JMJD2A), 435 nM (JMJD2B), 1100 nM (JMJD2C), 290 nM (JMJD2D), 340 nM (JMJD2E), 855 nM (JMJD3)
体外研究(In Vitro)	JIB-04 is consistently selective for cancer vs. normal cells, demonstrated by the higher sensitivity of lung and prostate cancer lines (with IC50 as low as 10 nM) compared to HBECs and PrSCs/PrECs. JIB-04 inhibits cellular Jumonji demethylase activity, and Jumonji levels affect JIB-04 action in cells. JIB-04 significantly inhibits the proliferation of GB cell lines and stem-enriched cultures. JIB-04 exerts its maximal inhibitory activity against KDM5A, and modulates the expression of genes involved in the control of cancer cell growth and leads to hypermethylation of H3K4. Furthermore, JIB-04 (2500 nM) activates the autophagy and apoptotic pathways and inactivates PI3K. JIB-04 also cooperates with TMZ in killing GB cells. has not independently confirmed the accuracy of these methods. They are for referen
体内研究(In Vivo)	JIB-04 results in a significant reduction in cancer-induced death rates in mice, prolonging survival. JIB-04 (60, 40 and 20 mg/kg, i.p.) reaches bioactive concentration in the brain of the mice. The orthotopic GB xenograft model shows a trend toward longer survival in JIB-04-treated mice with an Hazard Ratio of 0.5. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Wang L, et al. A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth. Nat Commun, 2013. 4: p. 2035. [2]. Banelli B, et al. Small molecules targeting histone demethylase genes (KDMs) inhibit growth of temozolomide-resistant glioblastoma cells. Oncotarget. 2017 Apr 4.

溶解度数据	In Vitro: DMSO : 50 mg/mL (161.94 mM; Need ultrasonic)Ethanol : 2 mg/mL (6.48 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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