A selective chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5; shows cellular target engagement with a pIC50 value of 7.7

GSK6853 – 10 mg

Brand:
Cayman
CAS:
1910124-24-1
Storage:
-20
UN-No:
Non-Hazardous - /

GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5.{33511} It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells.{33511} See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A selective chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5; shows cellular target engagement with a pIC50 value of 7.7

Formal name: N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide

Synonyms: 

Molecular weight: 409.5

CAS: 1910124-24-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains

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