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Key Documents

Safety Information

5.34354

Sigma-Aldrich

p300/CBP Inhibitor X, EML425

Synonym(s):

p300/CBP Inhibitor X, EML425, 1,3-dibenzyl-5-(4-hydroxy-2,6-dimethylbenzylidene)pyrimidine-2,4,6(1H,3H,5H)-trione, EML-425, p300/CBP Acetyltransferase Inhibitor, EML425

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400 μL
CN¥1,636.44

CN¥1,636.44

Available to ship onApril 17, 2025Details

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400 μL
CN¥1,636.44

About This Item

Empirical Formula (Hill Notation):
C27H24N2O4
Molecular Weight:
440.49
UNSPSC Code:
12352200
NACRES:
NA.77

CN¥1,636.44

Available to ship onApril 17, 2025Details

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Assay

≥98% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

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dTTP Lithium salt

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dTTP

GTP =98% (HPLC), solution, pkg of 400 μL (100 mM; 40 μmol)

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GTP

dCTP =98%, solution, 100 mM, suitable for DNA sequencing, suitable for DNA amplification

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Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

100

assay

97% (HPLC)

assay

≥98%

assay

98% (HPLC)

assay

98%

form

solution

form

solution

form

solution

form

solution

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

concentration

100 mM

concentration

100 mM

concentration

-

concentration

100 mM

General description

A cell-permeable benzylidenbarbituric acid derivative that acts as a potent, selective inhibitor of lysine acetyltransferase p300/CBP paralogues (IC50 = 2.9 µM and 1.1 µM for recombinant p300 and CBP, respectively). The inhibition appears to be reversible and is non-competitive with respect to both acetyl-CoA and a histone H3 peptide. It binds to both the free enzyme and the enzyme-substrate complex with uneven affinities. Does not affect the activity of general control non-derepressible 5 (GCN5) and p300/CBP-associated factor (PCAF). Shown to reduce the acetylation of lysine H4K5 and H3K9 in U937 cells (~100 µM) and induce a cell cycle arrest at the G0/G1 phase with an increase in the percentage of hypodiploid nuclei (~ 100 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
p300/CBP
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Milite, C., et al. 2015. J. Med. Chem.58, in press.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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