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252790 Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem

Histone Methyltransferase EZH2 Inhibitor, DZNep, CAS 120964-45-6, is a cell-permeable inhibitor of EZH2-mediated trimethylation of K27 on histone H3.

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

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

252790
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
120964-45-6C₁₂H₁₄N₄O₃ • HCl • H₂O

Products

Catalogue NumberPackaging Qty/Pack
252790-2MG Glass bottle 2 mg
Description
OverviewA 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. Also available as a 25 mM solution in H2O (Cat. No. 506069).
Catalogue Number252790
Brand Family Calbiochem®
Synonyms3-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
References
ReferencesFiscus, W., et al. 2009. Blood 13, 2733.
Product Information
CAS number120964-45-6
FormTan solid
FormulationSupplied as a hydrochloride salt.
Hill FormulaC₁₂H₁₄N₄O₃ • HCl • H₂O
Chemical formulaC₁₂H₁₄N₄O₃ • HCl • H₂O
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
252790-2MG 04055977217353

Documentation

Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Histone Methyltransferase EZH2 Inhibitor, DZNep - CAS 120964-45-6 - Calbiochem Certificates of Analysis

TitleLot Number
252790

References

Reference overview
Fiscus, W., et al. 2009. Blood 13, 2733.

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.

Revision19-February-2014 JSW
Synonyms3-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
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.
FormTan solid
FormulationSupplied as a hydrochloride salt.
Intert gas (Yes/No) Packaged under inert gas
CAS number120964-45-6
Chemical formulaC₁₂H₁₄N₄O₃ • HCl • H₂O
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesFiscus, W., et al. 2009. Blood 13, 2733.