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安全信息

5.34354

Sigma-Aldrich

p300/CBP Inhibitor X, EML425

别名:

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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About This Item

经验公式（希尔记法）:
C27H24N2O4
分子量:
440.49
UNSPSC代码:
12352200
NACRES:
NA.77
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方案

≥98% (HPLC)

质量水平

100

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

yellow

溶解性

DMSO: 100 mg/mL

储存温度

2-8°C

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1 of 4

此商品
124001110783111802
Spectromelt® A 20 lithium metaborate

112996

Spectromelt® A 20

Spectromelt® A 22 lithium metaborate/di-lithium tetraborate 22:12

124001

Spectromelt® A 22

Spectromelt® A 10 (di-lithium tetraborate)

110783

Spectromelt® A 10

Spectromelt® A 12 66% di-lithium tetraborate/34% lithium metaborate

111802

Spectromelt® A 12

solubility

water: soluble 141.2  g/L at 20 °C (68 °F)

solubility

-

solubility

141.2 g/L

solubility

50 g/L

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

grade

for X-ray fluorescence analysis

grade

-

grade

for X-ray fluorescence analysis

grade

for X-ray fluorescence analysis

mp

840 °C

mp

-

mp

930 °C

mp

-

cation traces

Ag: ≤5 ppm, Ba: ≤5 ppm, Cd: ≤5 ppm, Cr: ≤5 ppm, Fe: ≤10 ppm, K: ≤10 ppm, Mn: ≤5 ppm, Na: ≤5 ppm, Sr: ≤5 ppm, Al: ≤10, Co: ≤5 ppm, Ga: ≤5 ppm, Na: ≤20 ppm, Zn: ≤5 ppm, Ca: ≤20 ppm, Mg: ≤5 ppm, Cu: ≤5 ppm, Pb: ≤5 ppm

cation traces

-

cation traces

Ag: ≤5 ppm, Al: ≤10, Ba: ≤5 ppm, Ca: ≤20 ppm, Cd: ≤5 ppm, Co: ≤5 ppm, Cr: ≤5 ppm, Cu: ≤5 ppm, Fe: ≤10 ppm, Ga: ≤5 ppm, K: ≤10 ppm, Mg: ≤5 ppm, Mn: ≤5 ppm, Na: ≤20 ppm, Ni: ≤5 ppm, Pb: ≤5 ppm, Sr: ≤5 ppm, Zn: ≤5 ppm

cation traces

Ag: ≤5 ppm, Al: ≤10 ppm, Ba: ≤5 ppm, Ca: ≤20 ppm, Cd: ≤5 ppm, Co: ≤5 ppm, Cr: ≤5 ppm, Cu: ≤5 ppm, Fe: ≤10 ppm, Ga: ≤5 ppm, K: ≤10 ppm, Mg: ≤5 ppm, Mn: ≤5 ppm, Na: ≤20 ppm, Ni: ≤5 ppm, Pb: ≤5 ppm, Sr: ≤5 ppm, Zn: ≤5 ppm

一般描述

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.

生化/生理作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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