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500561 Ezh2 Inhibitor II, EI1 - CAS 1418308-27-6 - Calbiochem

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

Synonyms: 6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide, Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI

Primary Target: Ezh2/PRC2
500561
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1418308-27-6C₂₃H₂₆N₄O₂

Products

Catalogue NumberPackaging Qty/Pack
5.00561.0001 Glass bottle 10 mg
Description
OverviewA cell-permeable indolocarboxamide compound that acts as a potent and selective inhibitor against Ezh2/PRC2 (Polycomb repressive complex 2; Ezh2/SUZ12/EED/AEBP2/RbAP48) HMTase activity (IC50/substrate = 15 nM/H3K27me021-44 and 13 nM/H3K27me221-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1 µM) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC50 = 1.34 µM) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC50 >100 µM). Shown to suppress cellular H3K27 dimethylation and trimethylation (1 to 10 µM) in DLBCL cultures and exhibit antiproliferation activity against DLBCL cell lines with wt or mutant Ezh2 (3.3 µM to 10 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number500561
Brand Family Calbiochem®
Synonyms6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide, Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI
References
ReferencesQi, W., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 21360.
Product Information
CAS number1418308-27-6
FormWhite solid
Hill FormulaC₂₃H₂₆N₄O₂
Chemical formulaC₂₃H₂₆N₄O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetEzh2/PRC2
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 Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-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
5.00561.0001 04055977244953

Documentation

Ezh2 Inhibitor II, EI1 - CAS 1418308-27-6 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Qi, W., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 21360.
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.

Revision17-May-2013 JSW
Synonyms6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide, Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI
DescriptionA cell-permeable indolocarboxamide compound that acts as a potent and selective inhibitor against Ezh2/PRC2 (Polycomb repressive complex 2; Ezh2/SUZ12/EED/AEBP2/RbAP48) HMTase activity (IC50/substrate = 15 nM/H3K27me021-44 and 13 nM/H3K27me221-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1 µM) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC50 = 1.34 µM) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC50 >100 µM). Shown to selectively suppress cellular H3K27 dimethylation and trimethylation (1 to 10 µM in 1 to 5 days) in DLBCL (diffuse large B cell lymphoma) cultures, but not those of H3K4, H3K9, H3K36, or H3K79. EI1 is shown to exhibit antiproliferation activity against DLBCL cell lines with wt- (by 90% in G401 with 3.3 µM EI1; by 78% in Toledo with 10 µM EI1; 14 d incubation) or mutant- Ezh2 (by >96% in WSU-DLCL2/Y641F, SU-DHL6/Y641N, Karpas422/Y641N, and DB/Y641N cultures with 3.3 µM EI1; by >96% in SU-DHL4 cultures with10 µM EI1; 14 d incubation), while being less effective against MEF (by 40% in 11 days at 3.3 µM) and ineffective toward wt Ezh2-expressing GA10 and OCI-LY19.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1418308-27-6
Chemical formulaC₂₃H₂₆N₄O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesQi, W., et al. 2012. Proc. Natl. Acad. Sci. USA. 109, 21360.