Bromosporine

Catalog No.S7233 Batch:S723301

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Technical Data

Formula

C17H20N6O4S

Molecular Weight 404.44 CAS No. 1619994-69-2
Solubility (25°C)* In vitro DMSO 81 mg/mL (200.27 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.
Targets
CECR2 [1] BRD9 [1] BRD4 [1] BRD2 [1]
17 nM 0.122 μM 0.29 μM 0.41 μM
In vitro In cell-based assays, Bromosporine (1 µM) accelerates FRAP recovery of BRD4 and CREBBP, while shows no activities against TIF1α, BAZ2A, and SMARCA2 even at 10 µM. Bromosporine shows moderate cytotoxicity in HeLa cells at 18 µM. Bromosporine, as a chemical probe for bromodomain functional assays, will be very useful in elucidating further biological roles of reader domains. [2]

Protocol (from reference)

Selleck's Bromosporine has been cited by 6 publications

Discovery of Dual TAF1-ATR Inhibitors and Ligand-Induced Structural Changes of the TAF1 Tandem Bromodomain [ J Med Chem, 2022, 65(5):4182-4200] PubMed: 35191694
BPTF promotes the progression of distinct subtypes of breast cancer and is a therapeutic target [ Front Oncol, 2022, 12:1011173] PubMed: 36530982
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193
Insulin mutations impair beta-cell development in a patient-derived iPSC model of neonatal diabetes [ Elife, 2018, 7e38519] PubMed: 30412052
Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites [Chua MJ, et al. Int J Parasitol Drugs Drug Resist, 2018, 8(2):189-193] PubMed: 29631126
The bromodomain and extraterminal domain inhibitor bromosporine synergistically reactivates latent HIV-1 in latently infected cells. [ Oncotarget, 2017, 8(55):94104-94116] PubMed: 29212213

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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