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GSK 4027

Name: GSK 4027
Brand: TargetMol
SKU: T11495L
Rating: 4.5 (1 reviews)

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Catalog No. T11495LCas No. 2079896-25-4

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

GSK 4027

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Catalog No. T11495LCas No. 2079896-25-4

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.

Pack Size	Price	Availability	Quantity
1 mg	$268	35 days
5 mg	$589	35 days

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Product Introduction

Bioactivity

Description	GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. In a time-resolved fluorescence resonance energy transfer (TR-FRET) assay, it has a pIC50 of 7.4±0.11 for PCAF.
Targets&IC50	PCAF:(pic50)7.4±0.11
In vitro	The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel (pKi of 8.9 and 8.9 for PCAF and GCN5, respectively). GSK 4027 displays equipotent activity against PCAF and GCN5 (Ki: 1.4 nM for both bromodomains). GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. Due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full-length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC50 7.2 (IC50 60 nM)[1].

Chemical Properties

Molecular Weight	377.28
Formula	C₁₇H₂₁BrN₄O
Cas No.	2079896-25-4
Relative Density.	1.45 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 50 mg/mL (132.53 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6506 mL	13.2528 mL	26.5055 mL	132.5276 mL
5 mM	0.5301 mL	2.6506 mL	5.3011 mL	26.5055 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 mL	13.2528 mL
20 mM	0.1325 mL	0.6626 mL	1.3253 mL	6.6264 mL
50 mM	0.0530 mL	0.2651 mL	0.5301 mL	2.6506 mL
100 mM	0.0265 mL	0.1325 mL	0.2651 mL	1.3253 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

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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

Keywords

PCAFGSK-4027GSK4027GSK 4027