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Submit ReviewI-BRD9
Description: Potent and selective BRD9 inhibitor
Chemical Name: 5-Ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide
Purity: ≥98% (HPLC)
Biological Activity for I-BRD9
I-BRD9 is a potent and selective BRD9 inhibitor (pIC50 = 7.3). Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family. Downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the I-BRD9 probe summary on the SGC website.
External Portal Information for I-BRD9
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of I-BRD9 is reviewed on the chemical probes website.
Compound Libraries for I-BRD9
I-BRD9 is also offered as part of the Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for I-BRD9
| M. Wt | 497.55 |
| Formula | C22H22F3N3O3S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1714146-59-4 |
| PubChem ID | 91668541 |
| InChI Key | WRUWGLUCNBMGPS-UHFFFAOYSA-N |
| Smiles | O=C1C2=C(SC(C(NC3CCS(CC3)(=O)=O)=N)=C2)C(C4=CC=CC(C(F)(F)F)=C4)=CN1CC |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for I-BRD9
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.76 | 100 |
Preparing Stock Solutions for I-BRD9
The following data is based on the product molecular weight 497.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.01 mL | 10.05 mL | 20.1 mL |
| 5 mM | 0.4 mL | 2.01 mL | 4.02 mL |
| 10 mM | 0.2 mL | 1 mL | 2.01 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets for I-BRD9
References for I-BRD9
References are publications that support the biological activity of the product.
Theodoulou et al (2015) Discovery of I-BRD9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition. J.Med.Chem 59 1425 PMID: 25856009
If you know of a relevant reference for I-BRD9, please let us know.
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Keywords: I-BRD9, I-BRD9 supplier, bromodomains, containing, protein, extra, terminal, inhibits, inhibitors, potent, selective, downregulates, downregulation, sgc, structural, genomics, consortium, Bromodomains, 5591, Tocris Bioscience
5 Citations for I-BRD9
Citations are publications that use Tocris products. Selected citations for I-BRD9 include:
Nasun et al (2022) BRD9 regulates interferon-stimulated genes during macrophage activation via cooperation with BET protein BRD4. Proc Natl Acad Sci U S A 119 PMID: 34983841
Yong et al (2020) The bromodomain containing protein BRD-9 orchestrates RAD51-RAD54 complex formation and regulates homologous recombination-mediated repair. Nat Commun 11 2639 PMID: 32457312
Yili et al (2023) BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism. Nat Commun 14 1413 PMID: 36918560
Wei et al (2018) Vitamin D switches BAF complexes to protect β cells. Cell 173 1135 PMID: 29754817
Brien et al (2018) Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife 7 e41305 PMID: 30431433
Do you know of a great paper that uses I-BRD9 from Tocris? Please let us know.
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