Hersteller MedChem Express
Kategorie Produkte / Inhibitors
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mM*1mL (in DMSO)
ArtNr HY-12583-10mM
Eclass 6.1 30220300
Eclass 9.0 32160605
10 mM in DMSO
Biological Description
A-366 is a peptide-competitive inhibitor of G9a/GLP with an enzymatic IC50 of ca.3 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets.
IC50 value: 3 nM
Target: HMTase
in vitro: A-366 is a cell-active G9a/GLP small molecule inhibitor. The potency and selectivity of A-366 made it an ideal candidate to probe the cellular activities of G9a/GLP. A-366 reduced the total levels of H3K9me2 in a time and concentration dependent manner with a cellular EC50 of ca.300 nM. A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2. Additionally, the selectivity profile of A-366 has aided in the discovery of a potentially important role for G9a/GLP in maintenance of leukemia. Long term treatment of leukemia cell lines with A-366 results in differentiation and inhibition of growth
in vivo: Mice treated with A-366 administered via osmotic mini-pump at 30 mg/kg/day for two weeks showed no overt toxicity. Furthermore, treatment of a flank xenograft leukemia model with A-366 resulted in growth inhibition consistent with the profile of H3K9me2 reduction observed.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 133,57 €
Preis: 133,57 €

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