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Cat. No.: HY-122595

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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.

CAS No.: 1377997-28-8
Formula: C₂₇H₂₈ClN₅O₂
Molecular Weight:490.00

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (266 KB)

EZH2-IN-1 Chemical Structure

CAS No.: 1377997-28-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All Histone Methyltransferase Isoforms :

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]

Chemical Information

CAS No. 1377997-28-8
Molecular Weight 490.00
Formula C₂₇H₂₈ClN₅O₂
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Shivani Garapaty-Rao, et al.Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth. Chem Biol. 2013 Nov 21;20(11):1329-39. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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