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. In cell-based assays, Bromosporine (1 µM) accelerates FRAP recovery of BRD4 and CREBBP, while shows no activities against TIF1α, BAZ2A, and SMARCA2 (at 10 µM). Bromosporine shows moderate cytotoxicity in HeLa cells at 18 µM. It is a very useful chemical probe for bromodomain functional assays.
CAS Number: 1619994-69-2
Molecular Weight: 404.44
Chemical Name: ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
Bromosporine (1 μM) accelerates FRAP recovery of BRD4 and CREBBP, while shows no activities against TIF1α, BAZ2A, and SMARCA2 even at 10 μM. Bromosporine (18 μM) has moderate cytotoxicity in HeLa cells.
- 15th HELLENIC SYMPOSIUM OF MEDICINAL CHEMISTRY.
- Turky A, Bayoumi AH, Ghiaty A, El-Azab AS, A-M Abdel-Aziz A, Abulkhair HS. Design, synthesis, and antitumor activity of novel compounds based on 1, 2, 4-triazolophthalazine scaffold: Apoptosis-inductive and PCAF-inhibitory effects. Bioorg Chem. 2020 Aug;101:104019.
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