MilliporeSigma
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5.00561

Sigma-Aldrich

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

Synonym(s):
Ezh2 Inhibitor II, EI1 - CAS 1418308-27-6 - Calbiochem, Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI, 6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide
Empirical Formula (Hill Notation):
C23H26N4O2
CAS Number:
Molecular Weight:
390.48

assay

≥98% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL

storage temp.

2-8°C

General description

A 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 &gt96% in WSU-DLCL2/Y641F, SU-DHL6/Y641N, Karpas422/Y641N, and DB/Y641N cultures with 3.3 µM EI1; by &gt96% 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.
A 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.

Packaging

10 mg in Glass bottle
Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Ezh2/PRC2
Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Certificate of Analysis

Enter Lot Number to search for Certificate of Analysis (COA).

Certificate of Quality

Enter Lot Number to search for Certificate of Quality (COQ).

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