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506069 InSolution™ EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem

A 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep in H₂O.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 3-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

Primary Target: EZH2
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
120964-45-6C₁₂H₁₄N₄O₃ • HCl

Products

Catalog NumberPackaging Qty/Pack
5.06069.0001 Glass bottle 1 mg
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 number120964-45-6
FormLiquid
FormulationA 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H₂O.
Hill FormulaC₁₂H₁₄N₄O₃ • HCl
Chemical formulaC₁₂H₁₄N₄O₃ • HCl
ReversibleY
Quality LevelMQ100
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
Global Trade Item Number
Catalog Number GTIN
5.06069.0001 04055977243031

Documentation

InSolution™ EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem 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
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 number120964-45-6
Chemical formulaC₁₂H₁₄N₄O₃ • HCl
Purity≥98% by HPLC
Storage Protect from light
Avoid freeze/thaw
≤ -70°C
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.