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Product Name | Histone Methyltransferase EZH2 Inhibitor, DZNep |
Description | Purity ~97% (HPLC). A cell-permeable compound that is shown (at 1uM concentrations) to inhibit EZH2-mediated trimethylation of K27 on histone H3 and induces the expression of cell-cycle regulatory genes, p21 and p27, as well as the cell death regulator, FBXO32, in OCI-AML3 and HL-60 cells, whereby treatment with inhibitor increases p16 levels in the former, but not the latter of the two cultures. At concentrations between 200nM and 2000nM, this compound is found to dose-dependently deplete the expression of polycomb group proteins EZH2, SUZ12, and EED in cultured and primary AML cell extracts. At concentrations up to ≥ 1000nM, DZNep dose-dependently increases the percentage of apoptotic cells up to > ~ 38%, with greater potency against OCI-AML3 than HL-60 cultures and inhibits colony growth up to > ~ 85% for both cell lines. In OCI-AML3 cultures, 1000nM of treatment demonstrates a significant increase in the accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease i |
Size | 2mg |
Concentration | n/a |
Applications | n/a |
Other Names | Histone Methyltransferase EZH2 Inhibitor, DZNep (3-deazaneplanocin A, HCl, (1S,2R,5R)-5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol, HCl, HMTase Inhibitor X) |
Gene, Accession, CAS # | n/a |
Catalog # | 217432 |
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Order / More Info | Histone Methyltransferase EZH2 Inhibitor, DZNep from UNITED STATES BIOLOGICAL |
Product Specific References | n/a |
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