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EML 425

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Purity:100%

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COA LCMS HNMR

EML 425

Catalog No. T15216Cas No. 1675821-32-5

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

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Pack Size	Price	Availability
1 mg	$38	In Stock
5 mg	$89	In Stock
10 mg	$155	In Stock
25 mg	$336	In Stock
50 mg	$503	In Stock
100 mg	$732	In Stock
1 mL x 10 mM (in DMSO)	$98	In Stock

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Product Introduction

Bioactivity

Description

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

In vitro

EML 425 is shown to be a reversible inhibitor, noncompetitive versus both acetyl-CoA and a histone H3 peptide, and able to bind both the free enzyme and the enzyme-substrate complex, even with unequal affinity constants. EML 425, noncompetitive versus both acetyl-CoA and a histone H3 peptide, shows good cell permeability. EML 425 inhibits both p300 and CBP (IC50 values of 2.9 and 1.1 μM, respectively) while being practically inactive against the enzymes general control non-derepressible-5 (GCN5) and p300/CBP-associated factor (PCAF). EML 425 causes a marked and time-dependent reduction in the acetylation of lysine H4K5 and H3K9 in U937 cells. The binding site for EML 425 is an alternative pocket lying near the substrate lysine binding groove and close to the acetylation site[1].

Chemical Properties

Molecular Weight	440.49
Formula	C27H24N2O4
Cas No.	1675821-32-5

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (567.55 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2702 mL	11.3510 mL	22.7020 mL	113.5100 mL
5 mM	0.4540 mL	2.2702 mL	4.5404 mL	22.7020 mL
10 mM	0.2270 mL	1.1351 mL	2.2702 mL	11.3510 mL
20 mM	0.1135 mL	0.5675 mL	1.1351 mL	5.6755 mL
50 mM	0.0454 mL	0.2270 mL	0.4540 mL	2.2702 mL
100 mM	0.0227 mL	0.1135 mL	0.2270 mL	1.1351 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc