Home Epigenetics DNA/RNA Synthesis inhibitor GSK6853

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GSK6853 DNA/RNA Synthesis inhibitor

Cat.No.S8265

GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested.
GSK6853 DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 409.48

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Quality Control

Batch: S826501 DMSO]81 mg/mL]false]Ethanol]81 mg/mL]false]Water]Insoluble]false Purity: 99.44%
99.44

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (197.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 81 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
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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 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.

Chemical Information, Storage & Stability

Molecular Weight 409.48 Formula

C22H27N5O3

 Storage (From the date of receipt)
CAS No. 1910124-24-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1CNCCN1C2=CC3=C(C=C2NC(=O)C4=CC=CC=C4OC)N(C(=O)N3C)C

Mechanism of Action

Targets/IC50/Ki
BRPF1
(Cell-free assay)
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.
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.
References

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