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GSK6853

Catalog No.GC13025

BRPF1 inhibitor

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GSK6853 Chemical Structure

Cas No.: 1910124-24-1

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5mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

pIC50: 8.1

GSK6853 is a BRPF1 inhibitor.

The BRPF (Bromodomain and PHD Fingercontaining) protein family are key scaffolding proteins for assembly of MYST histone acetyltransferase complexes.

In vitro: In previous study, GSK6853 was tested in the BROMOscan panel of bromodomain binding assays and the results showed that consistent with the previous findings, it showed excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. In addition, screening GSK6853 against a panel of 48 unrelated assays revealed only off-target activities that were relatively weak compared to its high BRPF1 potency [1].

In vivo: To assess the suitability of GSK6853 for in vivo studies, its DMPK characteristics were studied in male CD1 mice by i.v., po, and i.p. administration. The results indicated that the i.p. route of administration would be suitable for dosing this molecule in further PK/PD models. Moreover, in order to be able to compare biochemical potency measurements to free blood concentrations, the fraction unbound in the CD1 mouse was also tested with a resulting value of 7.9% [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Bamborough, P. ,Barnett, H.A.,Becher, I., et al. GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain. ACS Med. Chem. Lett. 7(6), 552-557 (2016).

Chemical Properties

Cas No. 1910124-24-1 SDF
Chemical Name N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide
Canonical SMILES C[C@H](CNCC1)N1C2=C(NC(C3=CC=CC=C3OC)=O)C=C4C(N(C)C(N4C)=O)=C2
Formula C22H27N5O3 M.Wt 409.5
Solubility ≤30mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.442 mL 12.21 mL 24.42 mL
5 mM 0.4884 mL 2.442 mL 4.884 mL
10 mM 0.2442 mL 1.221 mL 2.442 mL
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 16 reference(s) in Google Scholar.)

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