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GSK-6853

SKU: orb1225815

Description

A potent, highly selective and cell-active BRPF1 bromodomain inhibitor with TR-FRET pIC50 of 8.1; displays>1600-fold selectivity over others bromodomains (BRPF2/3, BRD4 BD1/BD2); displaces NanoLuc-tagged BRPF1 bromodomain from Halo-tagged histone H3.3 (IC50=20 nM) and disrupts chromatin binding in cell assays; demonstrates properties suitable for cellular and in vivo studies.

Images & Validation

Key Properties

CAS Number1910124-24-1
MW409.4815
Purity>98% (HPLC)
FormulaC22H27N5O3
SMILESO=C(NC1=C(N2[C@H](C)CNCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
TargetBromodomain
SolubilityDMSO: ≥ 29 mg/mL

Bioactivity

In Vivo
The ip route of administration would be suitable for dosing GSK6853 in potential PK/PD models.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

GSK6853

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GSK-6853 (orb1225815)

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(Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
$ 80.00
5 mg
$ 110.00
10 mg
$ 170.00
25 mg
$ 280.00
50 mg
$ 470.00
100 mg
$ 710.00
500 mg
$ 1,500.00