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Cat. No.: HY-111544

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EML741

EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC₅₀ of 23 nM, K_d of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC₅₀, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.

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

CAS No.: 2328074-38-8
Formula: C₃₁H₄₉N₅O₂
Molecular Weight:523.75

Storage:

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

Data Sheet (270 KB)

EML741 Chemical Structure

CAS No.: 2328074-38-8

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

G9a

23 nM (IC₅₀)

G9a

1.13 μM (Kd)

DNMT1

3.1 μM (IC₅₀)

All Histone Methyltransferase Isoforms :

In Vitro

EML741 (Compound 12a) shows a similar high inhibition potency against G9a (97%, 98% inhibition at 10 μM and 25 μM, respectively) and GLP (95%, 98% inhibition at 10 μM and 25 μM, respectively)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Chemical Information

CAS No. 2328074-38-8
Molecular Weight 523.75
Formula C₃₁H₄₉N₅O₂
SMILES

COC1=C(OCCCN2CCCC2)C=C3N=C(C4CCCCC4)CN=C(NC5CCN(C(C)C)CC5)C3=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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]. Milite, et al. Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. J Med Chem. 2019 Mar 14;62(5):2666-2689. [Content Brief]

Calculators

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

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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.

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100 mg

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