1714146-59-4

1714146-59-4 structure

Name: I-BRD9
Chemical 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: 497.554
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-05-04 10:31:51
Modify Date: 2024-01-02 14:03:57
I-BRD9 is the first selective cellular chemical probe for BRD9 (pIC50=7.3).IC50 value: 7.3 (pIC50) [1]Target: BRD9in vitro: I-BRD9 is a selective cell active chemical probe for bromodomain containing protein 9 inhibition. I-BRD9, the first selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 is identified through structure-based design, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways and to the best of our knowledge, represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition.

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
Synonyms	Thieno[3,2-c]pyridine-2-carboximidamide, 5-ethyl-4,5-dihydro-4-oxo-N'-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]- 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 GSK602 I-BRD9

Description	I-BRD9 is the first selective cellular chemical probe for BRD9 (pIC50=7.3).IC50 value: 7.3 (pIC50) [1]Target: BRD9in vitro: I-BRD9 is a selective cell active chemical probe for bromodomain containing protein 9 inhibition. I-BRD9, the first selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 is identified through structure-based design, leading to greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways and to the best of our knowledge, represents the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Research Areas >> Cancer
References	[1]. Theodoulou NH, et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39.