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Chemical Structure| 1418308-27-6 Chemical Structure| 1418308-27-6

Structure of EI1
CAS No.: 1418308-27-6

Chemical Structure| 1418308-27-6

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EI1 is a selective inhibitor of wild type EZH2 and EZH2 Y641F mutant with IC50 values of 15 nM and 13 nM, respectively.

Synonyms: KB-145943

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Product Details of EI1

CAS No. :1418308-27-6
Formula : C23H26N4O2
M.W : 390.48
SMILES Code : CCC(CC)N(C=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C#N)=C2
Synonyms :
KB-145943
MDL No. :MFCD25976740
InChI Key :PFHDWRIVDDIFRP-UHFFFAOYSA-N
Pubchem ID :72199293

Safety of EI1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of EI1

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    EZH2 (Y641F), IC50:13 nM

    Ezh2 (wild-type), IC50:15 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
WSU-DLCL2 (Ezh2Y641F) 10 μM 4-5 days Inhibition of H3K27 methylation, leading to cell cycle arrest and apoptosis Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5
human dental pulp cells (hDPCs) 2 μM 24 and 48 hours EI1 upregulated the expression of ECM-related genes in hDPCs but failed to upregulate the COL1A1 protein level. In LPS-stimulated hDPCs, EI1 downregulated the expression of pro-inflammatory factors. J Dent Sci. 2024 Jan;19(1):177-185
KARPAS422 lymphoma cells 2 μM and 10 μM 60 days Investigated acquired resistance to EZH2 inhibitor EI1 in KARPAS422 cells, identifying two novel EZH2 mutations (Y111L and Y661D) conferring resistance. Oncogene. 2016 Feb 4;35(5):558-66
Huh-7.5 cells 0.012 μM 3 days To evaluate the inhibitory effect of EI-1 on HCVcc-1b/2a, results showed that EI-1 effectively inhibited HCVcc-1b/2a infection PLoS Pathog. 2010 Sep 2;6(9):e1001086
Huh-H1 cells 0.016 μM 3 days To evaluate the inhibitory effect of EI-1 on HCVpp-1b, results showed that EI-1 effectively inhibited HCVpp-1b infection PLoS Pathog. 2010 Sep 2;6(9):e1001086

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Rat pulpitis model Pulp capping 2 mM EI1 and 50 nM miR-181b-2-3p antagomir 7 days after surgery Compared to EI1 used alone, EI1 combined with the inhibitor upregulated the protein levels of COL1A1, FN1, and TGF-β2 in hDPCs, promoted hDPCs migration, and exhibited reparatory effects on inflamed rat pulp tissue. J Dent Sci. 2024 Jan;19(1):177-185

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.80mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL

References

 

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