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Art. -Nr.: HY-111589

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EPZ-4777

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1381761-52-9
Formel: C₂₇H₄₀N₈O₄
Molecular Weight:540.66

Speicherung:

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

Data Sheet (267 KB)

EPZ-4777 Chemical Structure

CAS. Nr.: 1381761-52-9

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	IC₅₀	1452 nM Compound: FED1	Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis Downregulation of H3K79 methylation in human MCF-10A cells by fluorescence microscopy analysis	[PMID: 23250418]
MOLM-13	EC₅₀	0.004 μM Compound: 18a, SYC-522	Antiproliferative activity against human MOLM13 cells containing MLL-AF9 Antiproliferative activity against human MOLM13 cells containing MLL-AF9	[PMID: 23879463]
MV4-11	EC₅₀	0.004 μM Compound: 18a, SYC-522	Antiproliferative activity against human MV4-11 cells containing MLL-AF4 Antiproliferative activity against human MV4-11 cells containing MLL-AF4	[PMID: 23879463]
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]
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]
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	0.004 μM Compound: 18a, SYC-522	Antiproliferative activity against human THP1 cells containing MLL-AF9 Antiproliferative activity against human THP1 cells containing MLL-AF9	[PMID: 23879463]
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.

Chemical Information

CAS. Nr. 1381761-52-9
Molecular Weight 540.66
Formel C₂₇H₄₀N₈O₄
SMILES

O[C@H]1[C@@H](O)[C@H](N2C=NC3=C2N=CN=C3N)O[C@@H]1CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 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)

Verweise

[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]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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