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GSK 525768A

Catalog No. T11472Cas No. 1260530-25-3

GSK 525768A, the inactive enantiomer of GSK525762A, exhibits no activity towards BET.

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Pack Size	Price	Availability
2 mg	$198	6-8 weeks
5 mg	$347	6-8 weeks
25 mg	$1,170	6-8 weeks
50 mg	$1,530	6-8 weeks
100 mg	$1,990	6-8 weeks
1 mL x 10 mM (in DMSO)	$382	6-8 weeks

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Questions

Product Introduction

Bioactivity

Description

GSK 525768A, the inactive enantiomer of GSK525762A, exhibits no activity towards BET.

In vitro

GSK 525768A interacts with the protein's module by establishing hydrogen bonds with the conserved asparagine residue, effectively mimicking the acetylated lysine's binding mechanism. This interaction leads to the compound's binding deeper within the acetylated lysine's binding site, all the while preserving the position of conserved water molecules in the acetyl-lysine binding cavity's base. GSK 525768A exhibits no activity towards BET and is identified as the (R)-enantiomer of GSK525762A. Contrasting its counterpart, GSK525762A, which influences the regulation of apolipoprotein A1 (APOA1) levels in liver cell assays, GSK 525768A does not impact APOA1 release, highlighting a distinctive functional divergence between the two enantiomers.

Chemical Properties

Molecular Weight	423.9
Formula	C22H22ClN5O2
Cas No.	1260530-25-3

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 100 mg/mL (235.90 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3590 mL	11.7952 mL	23.5905 mL	117.9523 mL
5 mM	0.4718 mL	2.3590 mL	4.7181 mL	23.5905 mL
10 mM	0.2359 mL	1.1795 mL	2.3590 mL	11.7952 mL
20 mM	0.1180 mL	0.5898 mL	1.1795 mL	5.8976 mL
50 mM	0.0472 mL	0.2359 mL	0.4718 mL	2.3590 mL
100 mM	0.0236 mL	0.1180 mL	0.2359 mL	1.1795 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

You can also refer to dose conversion for different animals. More

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