I-BRD9 is a potent, selective and cell permeable Bromodomain Containing Protein 9 (BRD9) inhibitor with Kd ~1.9 nM. It has >700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). It downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells. I-BRD9 is the first selective tool compound available to elucidate the cellular phenotype of BRD9 bromodomain inhibition.
CAS Number: 1714146-59-4
Molecular Weight: 497.55
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
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
I-BRD9 was used at 10 µM final concentration in vitro and in cellular assays.
- Theodoulou NH, et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. (2015) J Med Chem. In press.
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