506069 | InSolution™ EZH2 Inhibitor, DZNep - CAS 102052-95-9 - Calbiochem

506069
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₂H₁₄N₄O₃ • 3HCl; 2H2O 102052-95-9

      Pricing & Availability

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      5.06069.0001
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          Glass bottle 1 mg
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          Description
          Catalogue Number506069
          Brand Family Calbiochem®
          Synonyms3-Deazaneplanocin A, xHCl, yH₂O {x = 3 & y = 2}, (1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol, xHCl, yH₂O {x = 3 & y = 2}, NSC 617989
          References
          ReferencesSun, F., et al. 2009. Mol. Cancer Ther. 8, 3191.
          Miranda, T.B., et al. 2009. Mol. Cancer Ther. 8, 1579.
          Fiscus, W., et al. 2009. Blood 13, 2733.
          Tan, J., et al. 2007. Genes Dev. 21, 1050.
          Chiang, P.K., et al. 1992. J. Biol. Chem. 267, 4988.
          Tseng, C.K., et al. 1989. J. Med. Chem. 32, 1442.
          Glazer, R.I., et al. 1986. Biochem. Biophys. Res. Commun. 135, 688.
          Product Information
          CAS number102052-95-9
          FormLiquid
          FormulationA 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H₂O.
          Hill FormulaC₁₂H₁₄N₄O₃ • 3HCl; 2H2O
          Chemical formulaC₁₂H₁₄N₄O₃ • 3HCl; 2H2O
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetEZH2
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Dry Ice Only
          Toxicity Standard Handling
          Storage ≤ -70°C
          Protect from Light Protect from light
          Avoid freeze/thaw Avoid freeze/thaw
          Do not freeze Ok to freeze
          Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 monthst at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Sun, F., et al. 2009. Mol. Cancer Ther. 8, 3191.
          Miranda, T.B., et al. 2009. Mol. Cancer Ther. 8, 1579.
          Fiscus, W., et al. 2009. Blood 13, 2733.
          Tan, J., et al. 2007. Genes Dev. 21, 1050.
          Chiang, P.K., et al. 1992. J. Biol. Chem. 267, 4988.
          Tseng, C.K., et al. 1989. J. Med. Chem. 32, 1442.
          Glazer, R.I., et al. 1986. Biochem. Biophys. Res. Commun. 135, 688.

          Technical Info

          Title
          White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision10-January-2014 JSW
          Synonyms3-Deazaneplanocin A, xHCl, yH₂O {x = 3 & y = 2}, (1S,2R,5R)-5-(4-Amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol, xHCl, yH₂O {x = 3 & y = 2}, NSC 617989
          DescriptionA cell-permeable compound that is shown (at 1 µM 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 200 nm and 2000 nM, 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 ≥ 1000 nM, 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, 1000 nM 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), 200 nM 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.
          FormLiquid
          FormulationA 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H₂O.
          Intert gas (Yes/No) Packaged under inert gas
          CAS number102052-95-9
          Chemical formulaC₁₂H₁₄N₄O₃ • 3HCl; 2H2O
          Structure formulaStructure formula
          Purity≥98% by HPLC
          Storage ≤ -70°C
          Protect from light
          Avoid freeze/thaw
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 monthst at -20°C.
          Toxicity Standard Handling
          ReferencesSun, F., et al. 2009. Mol. Cancer Ther. 8, 3191.
          Miranda, T.B., et al. 2009. Mol. Cancer Ther. 8, 1579.
          Fiscus, W., et al. 2009. Blood 13, 2733.
          Tan, J., et al. 2007. Genes Dev. 21, 1050.
          Chiang, P.K., et al. 1992. J. Biol. Chem. 267, 4988.
          Tseng, C.K., et al. 1989. J. Med. Chem. 32, 1442.
          Glazer, R.I., et al. 1986. Biochem. Biophys. Res. Commun. 135, 688.