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), CAS [[102052-95-9]]

Product Overview

• Article Name: 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), CAS [[102052-95-9]]
• Biozol Catalog Number: USB-217432
• Supplier Catalog Number: 217432
• Alternative Catalog Number: USB-217432-2
• Manufacturer: US Biological
• Category: Biochemikalien

Product Description

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 in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle. When co-treated with panobinostat (PS), 200nM to 1000nM DZNep is shown to decrease cell viability in OCI-AML3 and HL-60 cultures more effectively than DZNep alone, in a dose-dependent manner. DZNep (1mg/kg, twice per week, i.p.) and PS significantly prolong the survival of mice implanted with HL-60 cells compared to treatment with either compound alone. DZNep is also a known S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitor. Synonyms: 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 CAS Number: 102052-95-9 Molecular Formula: C12H14N4O3 HCl H2O Solubility: DMSO Storage and Stability: Store at -20C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

Product Properties

• Purity: ~97% (HPLC)
• Form: Supplied as a hydrochloride salt.
• CAS Number: [102052-95-9]