5.09453

JHDM Inhibitor VII, JIB-04

• Sinônimo(s): JHDM Inhibitor VII, JIB-04, 5-Chloro-2-((2 E)-2-(phenyl(2-pyridinyl)methylene)hydrazino)pyridine, Histone Lysine Demethylase Inhibitor XIII, NSC693627, JIB04
• Fórmula empírica (Notação de Hill): C₁₇H₁₃ClN₄
• Número CAS: 199596-05-9
• Peso molecular: 308.76
• Código UNSPSC: 12352200

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: light beige
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: 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+
• chave InChI: YHHFKWKMXWRVTJ-OQKWZONESA-N

Descrição

Descrição geral

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).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Jumonji family of histone demethylases

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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.

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable