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EML425, CBP/p300 Inhibitor

EML425, CBP/p300 Inhibitor

$129.00
A selective, noncompetitive and cell permeable KAT3 histone acetyltransferases CBP/p300 inhibitor.
Catalog No. Unit Price Qty
M60257-2s 2 mg solid $129.00

Details

Product Information
Molecular Weight: 440.50
Formula: C27H24N2O4
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 50 mM
Chemical Name: 1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

EML425 is a selective, noncompetitive and cell permeable KAT3 histone acetyltransferases CBP/p300 inhibitor with IC50 of 1.1 µM for CBP and 2.9 µM for p300. It is noncompetitive versus both acetyl-CoA and a histone H3 peptide, and endowed with good cell permeability. In human leukemia U937 cells, EML425 induced a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9, a marked arrest in the G0/G1 phase and a significant increase in the hypodiploid nuclei percentage. EML425 may be an invaluable chemical probe not only for mechanistic studies of p300-mediated lysine acetylation but also to further investigate the biological role of this KAT enzyme and its implications in physiological and/or pathological processes.

How to Use:

In vitro: EML425 was used at 10-100 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

  • 1. Milite C, et al. A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach. (2015) J Med Chem. 58(6):2779-98. 



EML425_spec.pdf    
EML425_MSDS.pdf  

Products are for research use only. Not for human use. 

Description

Details

Product Information
Molecular Weight: 440.50
Formula: C27H24N2O4
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 50 mM
Chemical Name: 1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

EML425 is a selective, noncompetitive and cell permeable KAT3 histone acetyltransferases CBP/p300 inhibitor with IC50 of 1.1 µM for CBP and 2.9 µM for p300. It is noncompetitive versus both acetyl-CoA and a histone H3 peptide, and endowed with good cell permeability. In human leukemia U937 cells, EML425 induced a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9, a marked arrest in the G0/G1 phase and a significant increase in the hypodiploid nuclei percentage. EML425 may be an invaluable chemical probe not only for mechanistic studies of p300-mediated lysine acetylation but also to further investigate the biological role of this KAT enzyme and its implications in physiological and/or pathological processes.

How to Use:

In vitro: EML425 was used at 10-100 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

  • 1. Milite C, et al. A novel cell-permeable, selective, and noncompetitive inhibitor of KAT3 histone acetyltransferases from a combined molecular pruning/classical isosterism approach. (2015) J Med Chem. 58(6):2779-98. 



EML425_spec.pdf    
EML425_MSDS.pdf  

Products are for research use only. Not for human use. 

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