Chemical Name: 5-Chloro-2-[(E)-2-[phenyl(pyridin-2-yl)methylidene]hydrazin-1-yl]pyridine
Biological ActivityJIB 04 is a pan Jumonji histone demethylase inhibitor (IC50 values are 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively). Exhibits negligible activity at PHD2 and TET1. Selectively blocks cancer cell growth in vitro and diminishes tumor growth in H358 and A549 mouse xenograft models in vivo. Prolongs survival in a mouse model of breast cancer.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth.
Wang et al.
Nat. Commun., 2013;4:2035
Azinyl and diazinyl hydrazones derived from aryl N-heteroaryl ketones: synthesis and antiproliferative activity.
Grunicke and Hofmann
J. Med. Chem., 1997;40:4420
Citations for JIB 04
The citations listed below are publications that use Tocris products. Selected citations for JIB 04 include:
7 Citations: Showing 1 - 7
BIX01294 inhibits EGFR signaling in EGFR-mutant lung adenocarcinoma cells through a BCKDHA-mediated reduction in the EGFR level.
Authors: Jin Kyung Et al.
Exp Mol Med 2021;53:1877-1887
Inhibitor of growth protein 3 epigenetically silences endogenous retroviral elements and prevents innate immune activation.
Authors: Jan E Et al.
Nucleic Acids Res 2021;49:12706-12715
Heterochromatin-Driven Nuclear Softening Protects the Genome against Mechanical Stress-Induced Damage.
Authors: Jorge Et al.
Histone H3 K4/9/27 Trimethylation Levels Affect Wound Healing and Stem Cell Dynamics in Adult Skin.
Authors: Aiko Et al.
Stem Cell Reports 2020;14:34-48
H3K9 methyltransferases and demethylases control lung tumor-propagating cells and lung cancer progression.
Authors: Rowbotham Et al.
Nat Commun 2018;9:4559
Increasing G9a automethylation sensitizes B acute lymphoblastic leukemia cells to glucocorticoid-induced death.
Authors: Poulard Et al.
Cell Death Dis 2018;9:1038
Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis.
Authors: Lee Et al.
Nat Commun 2016;7:11278
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