EML741

Cat. No.: HY-111544: FAQs
Data Sheet Handling Instructions

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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.

EML741 Chemical Structure

CAS No. : 2328074-38-8

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•Related Small Molecules:

•Related Proteins:

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

IC₅₀ & Target^[1]

G9a

23 nM (IC₅₀)

G9a

1.13 μM (Kd)

DNMT1

3.1 μM (IC₅₀)

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.

Molecular Weight

523.75

Formula

C₃₁H₄₉N₅O₂

CAS No.

2328074-38-8

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.

Purity & Documentation

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]

EML741 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 *
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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:

EML7412328074-38-8EML 741EML-741Histone MethyltransferaseInhibitorinhibitorinhibit

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