1. Epigenetics
    Apoptosis
  2. Histone Methyltransferase
    Apoptosis
  3. EI1

EI1 (Synonyms: KB-145943)

Cat. No.: HY-15573 Purity: 99.74%
Handling Instructions

EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

For research use only. We do not sell to patients.

EI1 Chemical Structure

EI1 Chemical Structure

CAS No. : 1418308-27-6

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10 mM * 1 mL in DMSO USD 82 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
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10 mg USD 160 In-stock
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50 mg USD 480 In-stock
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100 mg USD 695 In-stock
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Description

EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

IC50 & Target[1]

EZH2 Y641F mutant type

13 nM (IC50)

EZH2 wild type

15 nM (IC50)

In Vitro

In DLBCL cells, EI1 (KB-145943) inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression. In mouse embryonic fibroblasts, EI1 (KB-145943) also inhibit H3K27me3 and cell proliferation. In addition, EI1 (KB-145943) selectively inhibits the growth of DLBCL cells carrying Ezh2 mutation, and causes cell cycle arrest and apoptosis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

390.48

Formula

C₂₃H₂₆N₄O₂

CAS No.

1418308-27-6

SMILES

CCC(CC)N(C=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C#N)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 7.69 mg/mL (19.69 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5610 mL 12.8048 mL 25.6095 mL
5 mM 0.5122 mL 2.5610 mL 5.1219 mL
10 mM 0.2561 mL 1.2805 mL 2.5610 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Exponentially growing diffused large B-cell lymphoma (DLBCL) cells are seeded in 12-well plates at a density of 1×105 cells/mL with the indicated concentration of EI1 (KB-145943). Viable cell number is determined every 3-4 d for up to 14 or 15 d by Vi-CELL. Mouse embryonic fibroblasts (MEFs) are seeded in a six-well plate at 2.5×104 cell/mL and treated with EI1 (KB-145943) (3.3 μM) or 4-OH-tamoxifen (100 nM). Viable cell number is determined at days 3, 6 and 11. On days of cell counts, fresh growth medium and compound are replenwashed and cells split back to a density of 1×105 cells/mL. Total cell number is expressed as split-adjusted viable cells per milliliter. IC50 is calculated by PRISM and all proliferation experiments are repeated more than two times and representative data are presented.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

EI1KB-145943EI 1EI-1KB145943KB 145943Histone MethyltransferaseApoptosisInhibitorinhibitorinhibit

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