Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

HomeProduct name listGSK6853

GSK6853

Synonym(s):(R)-N-(1,3-Dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide;N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide

  • CAS NO.:1910124-24-1
  • Empirical Formula: C22H27N5O3
  • Molecular Weight: 409.48
  • MDL number: MFCD30489734
  • Update Date: 2024-11-19 23:02:33
GSK6853 Structural

What is GSK6853?

Description

GSK6853 (1910124-24-1) is a very potent (pIC50 = 8.6 vs full length protein, 7.7 in cellular assays) inhibitor of Bromodomain and PHD Finger-containing 1 (BRPF1). It displayed >1600-fold selectivity over other bromodomains.

The Uses of GSK6853

N-[2,3-Dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide can be used in biological study of preparation of bromodomain and PHD finger-containing protein inhibitors.

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].

storage

Store at -20°C

References

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

Properties of GSK6853

Boiling point: 545.9±50.0 °C(Predicted)
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)
form  solid
pka 13.03±0.20(Predicted)
color  White
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.

Safety information for GSK6853

Computed Descriptors for GSK6853

Related products of tetrahydrofuran

You may like

  • GSK6853 CAS 1910124-24-1
    GSK6853 CAS 1910124-24-1
    1910124-24-1
    View Details
  • 1975-50-4 98%
    1975-50-4 98%
    1975-50-4
    View Details
  • 2-HYDROXY BENZYL ALCOHOL 98%
    2-HYDROXY BENZYL ALCOHOL 98%
    90-01-7
    View Details
  • 2-Chloro-1,3-Bis(Dimethylamino)Trimethinium  Hexafluorophosphate 221615-75-4 98%
    2-Chloro-1,3-Bis(Dimethylamino)Trimethinium Hexafluorophosphate 221615-75-4 98%
    221615-75-4
    View Details
  • 61397-56-6 CIS BROMO BENZOATE 98%
    61397-56-6 CIS BROMO BENZOATE 98%
    61397-56-6
    View Details
  • 14714-50-2 (2-Hydroxyphenyl)acetonitrile 98+
    14714-50-2 (2-Hydroxyphenyl)acetonitrile 98+
    14714-50-2
    View Details
  • 118753-70-1 98+
    118753-70-1 98+
    118753-70-1
    View Details
  • 733039-20-8 5-broMo-2-chloro-N-cyclopentylpyriMidin-4-aMine 98+
    733039-20-8 5-broMo-2-chloro-N-cyclopentylpyriMidin-4-aMine 98+
    733039-20-8
    View Details
Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.