Jumonji HDM Inhibitor, JIB-04 for cell activation

JIB-04 (E-isomer) is a potent, cell-permeable inhibitor of Jumonji histone demethylases in vitro and in vivo. (In vitro IC₅₀ values are 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively). JIB-04 is not a competitive inhibitor of α-ketoglutarate ; it selectively inhibits viability of several human cancer cell lines with little toxicity towards normal cells, and also diminishes tumor growth in xenograft mouse models.

N/A

199596-05-9

308.76

Biochemicals

5-Chloro-2-[(E)-2-[phenyl(pyridin-2​-yl)methylidene]hydrazin-1-yl]pyridine; NSC693627

C₁₇H₁₃ClN₄

White solid

N/A

No

Yes

≥98% by HPLC

DMSO (~20 mg/ml)

-20°C

gel pack

24 months

Protect from air and light

cell

For cells, cell lines and tissues in culture till half confluency.Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.