Name: I-BRD9
Price: 276.00 USD

- Overview
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    Background
    
    pIC50: 7.3I-BRD9 is a BRD9 inhibitor. BRD9 is identified as a bromodomain containing protein forming a small sub-branch of the bromodomain family tree. Human BRD9 has a single bromodomain and contains five isoforms which are produced by alternative splicing. In vitro: In previous study, the I-BRD9 development was driven by iterative medicinal chemistry, using structure based design to result in nanomolar potency at BRD9, over 700-fold selectivity against the BET family as well as more than 70-fold to a panel of 34 bromodomains. In Kasumi-1 cells, I-BRD9 could downregulate DUSP6, CLEC1, SAMSN1 and FES genes. Moreover, I-BRD9 was used to expore genes regulated by BRD9 in Kasumi-1 cells involved in immune response and oncology pathways. In addition, when BRD4 was used as a representative member of the BET family for initial selectivity screening, I-BRD9 was found to have a pIC50 of 5.3 against this protein. I-BRD9 thus represented the first available selective tool compound to investigate the cellular phenotype of the inhibition of BRD9 bromodomain [1]. In vivo: So far, there is no animal in vivo data reported for I-BRD9. Clinical trial: Up to now, I-BRD9 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    N-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-5-ethyl-4-oxo-7-(3-(trifluoromethyl)phenyl)-4,5-dihydrothieno[3,2-c]pyridine-2-carboximidamide
    
    CAS Number
    
    1714146-59-4
    
    Molecular Formula
    
    C22H22F3N3O3S2
    
    Molecular Weight
    
    497.55
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

I-BRD9

I-BRD9

Background

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