JIB-04

CAS No. 199596-05-9

JIB-04 ( JHDM Inhibitor VII | NSC 693627 )

Catalog No. M13115 CAS No. 199596-05-9

JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 39 In Stock
10MG 61 In Stock
25MG 82 In Stock
50MG 149 In Stock
100MG 259 In Stock
200MG 426 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    JIB-04
  • Note
    Research use only, not for human use.
  • Brief Description
    JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
  • Description
    JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively.
  • 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.
  • 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.
  • Synonyms
    JHDM Inhibitor VII | NSC 693627
  • Pathway
    Chromatin/Epigenetic
  • Target
    Histone Demethylase
  • Recptor
    JMJD2A| JMJD2B| JMJD2D| JMJD2E| JARID1A
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    199596-05-9
  • Formula Weight
    308.76
  • Molecular Formula
    C17H13ClN4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 25 mg/mL warmed (80.96 mM)
  • SMILES
    ClC1=CN=C(N/N=C(C2=CC=CC=C2)/C3=NC=CC=C3)C=C1
  • Chemical Name
    (E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Wang, L., et al. Nat Commun, 2013. 4: p. 2035.
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