2. Epigenetics
  3. Histone Methyltransferase
  4. EZH2-IN-1

EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research.

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

EZH2-IN-1 Chemical Structure

EZH2-IN-1 Chemical Structure

CAS No. : 1377997-28-8

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

EZH2-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research[1].

Cellular Effect
Cell Line Type Value Description References
HeLa EC50
7 μM
Compound: 23
Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method
Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method
[PMID: 25406853]
KARPAS-422 GI50
13.2 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 14 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 14 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
23 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 10 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 10 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
24.8 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 7 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 7 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
70 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 4 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 4 days by Cell-Titer luminescence assay
[PMID: 24900844]
KARPAS-422 GI50
9.1 μM
Compound: 44
Growth inhibition of human KARPAS422 cells after 17 days by Cell-Titer luminescence assay
Growth inhibition of human KARPAS422 cells after 17 days by Cell-Titer luminescence assay
[PMID: 24900844]
Molecular Weight

490.00

Formula

C27H28ClN5O2
CAS No.
SMILES

O=C(NC1CC(C)(C)NC(C)(C)C1)C2=CC=C(OC3=CC=CC(C4=CC=NN=C4)=C3C#N)C(Cl)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

EZH2-IN-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EZH2-IN-11377997-28-8Histone MethyltransferaseSAMEZH2EZH1EZH2wtEZH2 Y641N mutantH3K27me3H3K27me2diffuse large B cell lymphomaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EZH2-IN-1
Cat. No.:
HY-122595
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (0 KB) Français - FR (0 KB) Deutsch - DE (0 KB) Norwegian - NO (0 KB) Español - ES (0 KB) Swedish - SV (0 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.