Home Epigenetics Epigenetic Reader Domain inhibitor I-BRD9 For research use only.

I-BRD9

Synonyms: GSK602

I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.

I-BRD9 Chemical Structure

I-BRD9 Chemical Structure

CAS No. 1714146-59-4

Purity & Quality Control

I-BRD9 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Cell Data

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
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Biological Activity

Description I-BRD9 (GSK602) is a potent and selective BRD9 inhibitor with pIC50 of 7.3, while it displayed a pIC50 of 5.3 against BRD4.
Targets
BRD9 [1]
(Cell-free assay)		 BRD4 [1]
(Cell-free assay)
7.3(pIC50) 5.3(pIC50)
In vitro
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). 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[1].

Chemical Information & Solubility

Molecular Weight 497.55 Formula

C22H22F3N3O3S2
CAS No. 1714146-59-4 SDF Download I-BRD9 SDF
Smiles CCN1C=C(C2=C(C1=O)C=C(S2)C(=NC3CCS(=O)(=O)CC3)N)C4=CC(=CC=C4)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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