A pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50 values are 230

JIB-04 – 50 mg

Brand:
Cayman
CAS:
199596-05-9
Storage:
-20
UN-No:
Non-Hazardous - /

JIB-04 is a pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50s values = 230, 340, 435, 445, 855 and 1,100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3, and JMJD2C, respectively).{27169} It does not inhibit histone deacetylases and has minimal effect on the iron-containing enzymes methylcytosine dioxygenase TET1 and hypoxia-inducible factor prolyl hydroxylase 2.{27169} JIB-04 inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells but not in patient-matched normal cells.{27169,27168} It also inhibits Jumonji demethylase activity in cancer cells in vivo, resulting in reduced tumor burden and prolonged survival.{27169}  

 

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Description

A pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50 values are 230, 340, 435, 445, 855, and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C, respectively); inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells both in vitro and in vivo

Formal name: phenyl-2-pyridinyl-methanone, (E,E)-2-(5-chloro-2-pyridinyl)hydrazone

Synonyms:  JHDM Inhibitor VII|NSC 693627

Molecular weight: 308.8

CAS: 199596-05-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Demethylation

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