GSK6853
Uses- Product Name
- GSK6853
- CAS No.
- 1910124-24-1
- Chemical Name
- GSK6853
- Synonyms
- CS-2243;GSK6853;GSK-6853;GSK 6853;GSK6853 >=98% (HPLC);FQWDVNSBYDXPIO-CQSZACIVSA-N;BRPF1 bromodomain inhibitor GS6853;Inhibitor,inhibit,GSK6853,Epigenetic Reader Domain,GSK 6853,GSK-6853;N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxybenzamide;(R)-N-(1,3-Dimethyl-6-(2-methylpiperazin-1-yl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide;Benzamide, N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-
- CBNumber
- CB73145989
- Molecular Formula
- C22H27N5O3
- Formula Weight
- 409.48
- MOL File
- 1910124-24-1.mol
GSK6853 Property
- 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)
- pka
- 13.03±0.20(Predicted)
- form
- solid
- 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.
N-Bromosuccinimide Price
- Product number
- SML1985
- Product name
- GSK6853
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $115
- Updated
- 2023/06/20
- Product number
- SML1985
- Product name
- GSK6853
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $371
- Updated
- 2023/06/20
- Product number
- 20985
- Product name
- GSK6853
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 20985
- Product name
- GSK6853
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- 20985
- Product name
- GSK6853
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $169
- Updated
- 2024/03/01
GSK6853 Chemical Properties,Usage,Production
Uses
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.
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.
Uses
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
GSK6853 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from GSK6853 manufacturers
- Product
- GSK6853 1910124-24-1
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 97%-99.9%
- Supply Ability
- 100kg
- Release date
- 2019-12-25