BRPF1-IN-3( GSK-5959 | GSK 5959 | GSK5959. )

Catalog No. M16481 CAS No. 901245-65-6

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

BRPF1-IN-3
Note

Research use only, not for human use.
Brief Description

BRPF1-IN-3 is a potent, selective, membrane permeable BRPF1 bromodomain inhibitor with pIC50 of 7.1.
Description

BRPF1-IN-3 is a potent, selective, membrane permeable BRPF1 bromodomain inhibitor with pIC50 of 7.1; shows 100- and >1000-fold selectivity over BRPF2 and BRPF3, respectively; exhibits an IC50 of 0.98 uM in cellular protein interaction assay (displacement of NanoLuc-tagged BRPF1 bromodomain from Halo-tagged histone H3.3).
In Vitro

GSK-5959 (3a) also displays selectivity over the closely related family members, BRPF2 (100-fold) and BRPF3 (>1000-fold).GSK-5959 (3a) exhibits an EC50 = 0.98 μM) in cellular NanoBRET assay.GSK-5959 has no effect on TRIM24 SUMOylation.
In Vivo

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Synonyms

GSK-5959 | GSK 5959 | GSK5959.
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

BRPF1
Research Area

Other Indications
Indication

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CAS Number

901245-65-6
Formula Weight

394.475
Molecular Formula

C22H26N4O3
Purity

>98% (HPLC)
Solubility

DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )
SMILES

O=C(NC1=C(N2CCCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC
Chemical Name

N-(1,3-dimethyl-2-oxo-6-(piperidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide