EPZ-4777

Cat. No.: HY-111589: FAQs
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EPZ-4777 is a selective DOT1L inhibitor which inhibits H3K79 methylation in cancer cells, blocks the expression of leukemogenic genes, and selectively kills cells that contain the translocation. EPZ-4777 can be used for cancer research.

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

EPZ-4777 Chemical Structure

CAS No. : 1381761-52-9

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	0.2 μM Compound: 4	Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis	[PMID: 23795283]
MV4-11	EC₅₀	4.4 μM Compound: 55	Cytotoxicity against human MV4-11 cells harboring MLL-AF4 oncogene after 20 days by XTT assay Cytotoxicity against human MV4-11 cells harboring MLL-AF4 oncogene after 20 days by XTT assay	[PMID: 22924785]
NB-4	EC₅₀	101 μM Compound: 55	Cytotoxicity against human NB4 cells harboring wild type MLL oncogene after 20 days by XTT assay Cytotoxicity against human NB4 cells harboring wild type MLL oncogene after 20 days by XTT assay	[PMID: 22924785]
THP-1	EC₅₀	8.1 μM Compound: 55	Cytotoxicity against human THP1 cells harboring MLL-AF9 oncogene after 20 days by XTT assay Cytotoxicity against human THP1 cells harboring MLL-AF9 oncogene after 20 days by XTT assay	[PMID: 22924785]

In Vitro

EPZ-4777 (1-10000 nM, 24, 72 h) inhibits HOXA9 and LSD1 expression does and time-dependently in MOLM-13 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

540.66

Formula

C₂₇H₄₀N₈O₄

CAS No.

1381761-52-9

SMILES

O[C@@H]([C@H]([C@H](N1C=NC2=C1N=CN=C2N)O3)O)[C@H]3CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C

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]. Bon C, et al. Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein. Molecules. 2021 Aug 31;26(17):5300. [Content Brief]

[2]. Lillico R, et al. Selective DOT1L, LSD1, and HDAC Class I Inhibitors Reduce HOXA9 Expression in MLL-AF9 Rearranged Leukemia Cells, But Dysregulate the Expression of Many Histone-Modifying Enzymes. J Proteome Res. 2018 Aug 3;17(8):2657-2667. [Content Brief]

EPZ-4777 Related Classifications

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The molarity calculator equation

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

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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:

EPZ-47771381761-52-9EPZ4777EPZ 4777OthersDOT1LH3K79 methylationleukemogenic genecancerInhibitorinhibitorinhibit

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