5.09453

JHDM Inhibitor VII, JIB-04

• 别名: JHDM Inhibitor VII, JIB-04, 5-Chloro-2-((2 E)-2-(phenyl(2-pyridinyl)methylene)hydrazino)pyridine, Histone Lysine Demethylase Inhibitor XIII, NSC693627, JIB04
• 经验公式（希尔记法）: C₁₇H₁₃ClN₄
• CAS号: 199596-05-9
• 分子量: 308.76
• 分類程式碼代碼: 12352200

属性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: light beige
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C
• 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+
• InChI 密鑰: YHHFKWKMXWRVTJ-OQKWZONESA-N

说明

一般說明

The (E)-isomer of a cell-permeable pyridine hydrazone compound that acts as a selective inhibitor against Jumonji family histone demethylases (IC₅₀ = 230, 290-320, 340, 435, 445, 855, and 1,100 nM, respectively, against JARID1A/KDM5A, JMJD2D/KDM4D, JMJD2E/KDM4E, JMJD2B/KDM4B, JMJD2A/KMD4A, JMJD3/KDM6B, and JMJD2C/KDM4C, respectively), presumably via catalytic site iron interaction, displaying little or no potency toward 5mC DNA hydroxylase TET1, aurora kinases, HDACs, HIF prolyl hydroxylase PHD2, histone methyltransferases, protein arginine methyltransferases, sirtuins, or the non-jumonji family histone demethylase LSD1/KDM1A. Shown to exhibit anticancer activity against H358 and A549 lunger cancer cells both in cultures in vitro (IC₅₀ = 100 and 250 nM, respectively, in 4 d by MTS assays) and in mice in vivo (via i.p. at 100 mg/kg and p.o. at 55 mg/kg, respectively; 2-3 times per week).

The E-isomer of a cell-permeable pyridine hydrazone compound that acts as a selective inhibitor against Jumonji family histone demethylases (IC₅₀ = 230, 290-320, 340, 435, 445, 855, and 1,100 nM, respectively, against JARID1A/KDM5A, JMJD2D/KDM4D, JMJD2E/KDM4E, JMJD2B/KDM4B, JMJD2A/KMD4A, JMJD3/KDM6B, and JMJD2C/KDM4C, respectively), presumably via catalytic site iron interaction, displaying little toward 5mC DNA hydroxylase TET1, aurora kinases, HDACs, HIF prolyl hydroxylase PHD2, histone methyltransferases, protein arginine methyltransferases, sirtuins, or the non-jumonji family histone demethylase LSD1/KDM1A. Shown to exhibit anticancer activity against H358 and A549 lunger cancer cells both in cultures in vitro (IC₅₀ in 4 d = 100 and 250 nM, respectively) and in mice in vivo (via i.p. at 100 mg/kg and p.o. at 55 mg/kg, respectively; 2-3 times per week).

生化／生理作用

Cell permeable: yes

Primary Target
Jumonji family of histone demethylases

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Use only fresh DMSO for reconstitution.

其他說明

Wang, L., et al. 2013. Nat. Commun.4, 2035.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable