Home Epigenetics Epigenetic Reader Domain inhibitor I-BRD9

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I-BRD9 Epigenetic Reader Domain inhibitor

Cat.No.S7835

I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while this compound displayed a pIC50 of 5.3 against BRD4.
I-BRD9 Epigenetic Reader Domain inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 497.55

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Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUT78 Function assay 45 mins Inhibition of BRD9 in human HUT78 cells incubated for 45 mins by chemoproteomic competition binding assay, IC50 = 0.07943 μM. 25856009
HEK293 Function assay 18 hrs Binding affinity to BRD9 (amino acids 120-240) (unknown origin) assessed as displacememnt of NanoLuc-tagged BRD9 from Halo-tagged histone H3.3 expressed in HEK293 cells after 18 hrs by NanoBRET assay in presence of furimazine, IC50 = 0.15849 μM. 25856009
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 497.55 Formula

C22H22F3N3O3S2

 Storage (From the date of receipt)
CAS No. 1714146-59-4 Download SDF Storage of Stock Solutions

Synonyms GSK602 Smiles CCN1C=C(C2=C(C1=O)C=C(S2)C(=NC3CCS(=O)(=O)CC3)N)C4=CC(=CC=C4)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 99 mg/mL ( (198.97 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
BRD9 [1]
(Cell-free assay)
7.3(pIC50)
BRD4 [1]
(Cell-free assay)
5.3(pIC50)
In vitro
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). This compound 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[1].
References

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