I-BRD9, Bromodomain Containing Protein 9 (BRD9) Inhibitor

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.

Product information

CAS Number: 1714146-59-4

Molecular Weight: 497.55

Formula: C22H22F3N3O3S2

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

Smiles: CCN1C=C(C2SC(=CC=2C1=O)C(=N)NC1CCS(=O)(=O)CC1)C1=CC(=CC=C1)C(F)(F)F

InChiKey: WRUWGLUCNBMGPS-UHFFFAOYSA-N

InChi: InChI=1S/C22H22F3N3O3S2/c1-2-28-12-17(13-4-3-5-14(10-13)22(23,24)25)19-16(21(28)29)11-18(32-19)20(26)27-15-6-8-33(30,31)9-7-15/h3-5,10-12,15H,2,6-9H2,1H3,(H2,26,27)

Technical Data

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: ≥12 months 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

In Vitro:

I-BRD9 was used at 10 µM final concentration in vitro and in cellular assays.

References:

1. 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.

Products are for research use only. Not for human use.

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