1910124-24-1

Basic information

• Product Name: GSK6853
• Synonyms: GSK6853
• CAS NO: 1910124-24-1
• Molecular Formula: C22H27N5O3
• Molecular Weight: 409.48148
• EINECS: -0
• Product Categories: API
• Mol File: 1910124-24-1.mol

Chemical Properties

• Boiling Point: 545.9±50.0 °C(Predicted)
• Appearance: /
• Density: 1.247±0.06 g/cm3(Predicted)
• Storage Temp.: Sealed in dry,Store in freezer, under -20°C
• Solubility: Soluble in DMSO (25 mg/ml); ethanol (25 mg/ml)
• PKA: 13.03±0.20(Predicted)
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
• CAS DataBase Reference: GSK6853(CAS DataBase Reference)
• NIST Chemistry Reference: GSK6853(1910124-24-1)
• EPA Substance Registry System: GSK6853(1910124-24-1)

Safety Data

• Hazardous Substances Data: 1910124-24-1(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
GSK6853 is used as a bromodomain and PHD finger-containing protein inhibitor for its potential role in the biological study and development of novel therapeutics targeting BRPF1. Its high potency and selectivity make it a valuable compound for research and drug development in this area.
Used in Biological Research:
GSK6853 is used as a research tool in the study of bromodomain and PHD finger-containing proteins, particularly BRPF1. Its ability to selectively inhibit BRPF1 can help researchers understand the role of this protein in various biological processes and diseases, potentially leading to the discovery of new treatment options.

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].

References

Bamborough et al. (2016), GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain; ACS Med.Chem. Lett. 7 552

Relevant articles and documents

1,3-DIMETHYLBENZIMIDAZOLONE DERIVATIVE AS AN INHIBITOR OF THE BRPF1 BROMODOMAIN

A novel benzoimidazolyl compound, pharmaceutical compositions containing such a compound and its use in therapy.

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engag