Name: JIB-04
Price: 236.00 USD

- Overview
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    Background
    
    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].
    
    [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.
- Properties
  - Categories
    
    Jumonji histone demethylase inihibitor
    
    Alternative Name
    
    5-chloro-N-[(E)-[phenyl(pyridin-2-yl)methylidene]amino]pyridin-2-amine
    
    CAS Number
    
    199596-05-9
    
    Molecular Formula
    
    C17H13ClN4
    
    Molecular Weight
    
    308.76
    
    Purity
    
    98.50%
    
    Solubility
    
    insoluble in H2O; ≥14.2 mg/mL in DMSO; ≥2.83 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1=CC=C(C=C1)C(=NNC2=NC=C(C=C2)Cl)C3=CC=CC=N3
    
    * For Research Use Only
- Reference
  - 1. Parrish JK, McCann TS, et al. "The Jumonji-domain histone demethylase inhibitor JIB-04 deregulates oncogenic programs and increases DNA damage in Ewing Sarcoma, resulting in impaired cell proliferation and survival, and reduced tumor growth." Oncotarget. 2018 Sep 4;9(69):33110-33123. PMID:30237855

Documents

COA (Certificate Of Analysis)

HPLC

NMR (Nuclear Magnetic Resonance)

MSDS (Material Safety Data Sheet)

Datasheet

JIB-04

JIB-04

Background

Documents

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