Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM

PFI-3 – 25 mg

Brand:
Cayman
CAS:
1819363-80-8
Storage:
-20
UN-No:
Non-Hazardous - /

The SWI/SNF-related, Matrix-associated, Actin-dependent Regulator of Chromatin (SMARC) proteins integrate into complexes that remodel chromatin.{25296} The SMARC family A (SMARCA) members SMARCA2 (also known as BRM) and SMARCA4 (BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins.{25295,25294} The protein polybromo-1 (PB1, BRG1-associated factor) contains six bromodomains, but only the fifth (PB1(5)) shares the same structural signature as those of SMARCA2 and SMARCA4.{25295} PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. Evaluation of interactions of PFI-3 with different classes of bromodomains using thermal stability assay indicates that PFI-3 interacts selectively with bromodomains from SMARCA2 and SMARCA4 as well as the fifth domain of PB1. Similarly, PFI-1 (Item No. 11155) does not interact with a panel of kinases. See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases

Formal name: (2E)-1-(2-hydroxyphenyl)-3-[(1R,4R)-5-(2-pyridinyl)-2,5-diazabicyclo[2.2.1]hept-2-yl]-2-propen-1-one

Synonyms: 

Molecular weight: 321.4

CAS: 1819363-80-8

Purity: ≥98%

Formulation: A crystalline solid

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

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