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GSK6853

Catalog No. T3311 CAS 1910124-24-1

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

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GSK6853, CAS 1910124-24-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 59.00
10 mg	In stock	$ 109.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 343.00
100 mg	In stock	$ 531.00
500 mg	In stock	$ 1,150.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 99.11%

Purity: 99.08%

Purity: 99%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Molecular Weight	409.48
Formula	C22H27N5O3
CAS No.	1910124-24-1

Storage

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

Solubility Information

DMSO: 55 mg/mL (134.41 mM)

Ethanol: 81 mg/mL (197.81 mM)

References and Literature

1. Bamborough P, et al. ACS Med Chem Lett. 2016, 7(6):552-7.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library Anti-Aging Compound Library Epigenetics Compound Library NO PAINS Compound Library Bioactive Compound Library Chromatin Modification Compound Library PPI Inhibitor Library Histone Modification Compound Library Reprogramming Compound Library

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

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
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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

GSK6853 1910124-24-1 Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor inhibit GSK 6853 GSK-6853 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.