Bromosporine

Modify Date: 2024-01-02 19:12:41

Bromosporine Structure
Bromosporine structure
Common Name Bromosporine
CAS Number 1619994-69-2 Molecular Weight 404.444
Density 1.5±0.1 g/cm3 Boiling Point N/A
Molecular Formula C17H20N6O4S Melting Point N/A
MSDS Chinese USA Flash Point N/A

 Use of Bromosporine


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.IC50 value: 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2) [1]Target: BRD inhibitorIn 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.

 Names

Name ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate
Synonym More Synonyms

 Bromosporine 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.IC50 value: 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2) [1]Target: BRD inhibitorIn 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.
Related Catalog
References

[1]. 15th HELLENIC SYMPOSIUM OF MEDICINAL CHEMISTRY.

[2]. Bromosporine

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Molecular Formula C17H20N6O4S
Molecular Weight 404.444
Exact Mass 404.126678
PSA 135.96000
LogP 1.21
Index of Refraction 1.677
Storage condition 2-8°C

 Synonyms

Bromosporine
Ethyl (3-methyl-6-{4-methyl-3-[(methylsulfonyl)amino]phenyl}[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate
Carbamic acid, N-[3-methyl-6-[4-methyl-3-[(methylsulfonyl)amino]phenyl]-1,2,4-triazolo[4,3-b]pyridazin-8-yl]-, ethyl ester
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