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GSK6853

Name: GSK6853
Brand: TargetMol
SKU: T3311
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T3311Cas No. 1910124-24-1

GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.

GSK6853

🥰Excellent

Purity: 99.21%

Catalog No. T3311Cas No. 1910124-24-1

GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$35	In Stock	In Stock
10 mg	$65	In Stock	In Stock
25 mg	$118	In Stock	In Stock
50 mg	$198	In Stock	In Stock
100 mg	$319	In Stock	In Stock
200 mg	$453	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$32	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

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Purity:99.21%

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.
Targets&IC50	BRPF1:8.1(pIC50)
In vitro	Screening GSK6853 against a panel of 48 unrelated assays reveals only off-target activities that are relatively weak compared to the BRPF1 potency. However, to minimize the chance of off-target effects , the recommended concentration is no higher than 1 μM in cell-based assays[1].
In vivo	In male CD1 mouse, following IV administration (1 mg/kg), GSK6853 demonstrates a high blood clearance of 107 mL/min/kg, a moderate volume of distribution (5.5 L/kg) and a moderate terminal half-life of 1.7 h. Oral administration (PO, 3 mg/kg) achieves a moderate systemic exposure, with a Cmax of 42 ng/mL and Tmax of 1.5 h, resulting in a bioavailability of 22%. The intraperitoneal route of administration (IP, 3 mg/kg) reaches a Cmax of 469 ng/mL and Tmax of 0.25 h, resulting in a bioavailability of 85%. The results indicate that the IP route of administration would be suitable for dosing this molecule in potential PKPD models[1].

Chemical Properties

Molecular Weight	409.48
Formula	C₂₂H₂₇N₅O₃
Cas No.	1910124-24-1
Smiles	COc1ccccc1C(=O)Nc1cc2n(C)c(=O)n(C)c2cc1N1CCNC[C@H]1C
Relative Density.	1.247 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 55 mg/mL (134.32 mM), Sonication is recommended.

Ethanol: 81 mg/mL (197.81 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.88 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.4421 mL	12.2106 mL	24.4212 mL	122.1061 mL
5 mM	0.4884 mL	2.4421 mL	4.8842 mL	24.4212 mL
10 mM	0.2442 mL	1.2211 mL	2.4421 mL	12.2106 mL
20 mM	0.1221 mL	0.6105 mL	1.2211 mL	6.1053 mL
50 mM	0.0488 mL	0.2442 mL	0.4884 mL	2.4421 mL
100 mM	0.0244 mL	0.1221 mL	0.2442 mL	1.2211 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% Saline/PBS/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 μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

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

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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

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