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Long awaited highly potent, selective and cell permeable JARID1 (KDM5) histone demethylase inhibitor – KDM5-C49 and KDM5-C70

Jun 06,2013 02:45  |  news

Due to overwhelming inquiries from the research community, Xcess Biosciences is now offering the long awaited highly potent, selective and cell permeable JARID1 (KDM5) histone demethylase inhibitor  – KDM5-C49 and KDM5-C70, to study a selective subset of Jumonji histone demethylases, including stem cell and development, cancers, and neurological diseases.
 
 
KDM5-C49 is a potent and selective inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. It has IC50 <1 µM for KDM5 (or JARID1C) and UTX in histone lysine demethylase AlphaLISA assays, very good selectivity over JMJD1B, JMJD2A, JMJD2B and JMJD3 etc.  The highly polar carboxylate group of KDM5-C49 restricts its cellular permeability, so it has IC50 >1 µM for inhibiting demthylation of H3K4 in U2OS human osteosarcoma cell line and in human breast adenocarcinoma MCF7 tumor cell proliferation assay.
 
 
KDM5-C70 is a methyl ester derivative of KDM5-C49, developed as a pro-drug, masking the polarity of the acid group of the KDM5-C49, for cellular assays and in vivo use. It has IC50 <1 µM for KDM5B (or PLU1) and UTX in histone lysine demethylase AlphaLISA assays, very good selectivity over JMJD1B, JMJD2A, JMJD2B and JMJD3.  It has IC50 <1 µM for inhibiting demthylation of H3K4 in U2OS human osteosarcoma cell line. KDM5-C70 also suppresses human breast adenocarcinoma MCF7 tumor cell proliferation with IC50< 1 µM.   
 
 
In addition to KDM5-C49/KDM5-C70, there are the other Jumonji histone demethylase inhibitors available:
  • SD70 is a potent, selective and cell-permeable inhibitor of JMJD2 (KDM4C) histone demethylase.
  • ML324 is a potent, selective and cell permeable inhibitor of JMJD2E histone demethylase. 
  • IOX1 is a cell-permeable broad-spectrum inhibitor of most 2OG oxygenases, including histone demethylase JMJD3, JMJD1A, JMJD2A, JMJD2E, JMJD2C and UTX.
  • PBIT is a specific, reversible and cell-permeable inhibitor of JARID1B histone demethylases with μM activity.
  • JIB-04 (NSC693627, E-isomer) is a potent, selective and cell permeable pan Jumonji histone demethylase inhibitor.
  • GSK-J1 and its ethyl ester derivative GSK-J4 are the first selective and potent inhibitors of the H3K27 demethylases UTX and JMJD3. 
 
 
How to order: Xcess Biosciences, a premier reagent and service company, provides compounds in 10 mM DMSO solution and up to grams solid form. Please visit our website for order information, and other innovative products. Especially Xcess Biosciences continues to add more novel small molecule chemical probes to our Epigenetic Modulator Tool Box(right now we offer 71 unique compounds). Some newly add-in compounds are:
  • Remodelin  - First available Acetyl-transferase NAT10 inhibitor for laminopathies and aging.
  • IDH2-C100  - the potent, selective and cell permeable inhibitor of IDH2 R140Q and R172K mutant.
  • OTX-015 – a novel, highly potent, selective and cell permeable BET inhibitor in clinical trials.
  • BETP - positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor.
 
 
Xcess Biosciences also started to offer high quality, low price and bulk quantity of widely used growth factors and primary antibodies for epigenetics research (we offer free samples for your trial, please email or call us to get them).
 
 
Reference:
  1. Marc Labelle, et al. Inhibitors of Histone Demethylases. (2014) PCT WO 2014053491
  2. Peter Staller, et al. The Potential Applications of Enzymatic Inhibitors of KDM5 in Oncology. (2014) 21st Mol Med Tri-Conf (San Francisco).