For research use only. Not for therapeutic Use.
Bromosporine（Cat No.:I002078） is a potent inhibitor that targets bromodomains, which are protein modules involved in recognizing and binding acetylated lysine residues. It exhibits broad-spectrum inhibitory activity against various bromodomain-containing proteins. Bromosporine displays IC50 values of 0.41 μM, 0.29 μM, 0.122 μM, and 0.017 μM for BRD2, BRD4, BRD9, and CECR2, respectively. These findings highlight the potential of bromosporine as a valuable tool in bromodomain research and as a starting point for the development of novel therapeutics targeting bromodomain-containing proteins, including those involved in epigenetic regulation and disease-related processes.
| Catalog Number | I002078 |
| CAS Number | 1619994-69-2 |
| Synonyms | ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate |
| Molecular Formula | C17H20N6O4S |
| Purity | ≥95% |
| Target | Epigenetic Reader Domain; Apoptosis; CDK; HIV |
| Solubility | DMSO: ≥ 51.7 mg/mL |
| Storage | Store at -20°C |
| IC50 | 0.41/0.29/0.122/0.017 uM (BRD2/BRD4/BRD9/CECR2) |
| IUPAC Name | ethyl N-[6-[3-(methanesulfonamido)-4-methylphenyl]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate |
| InChI | InChI=1S/C17H20N6O4S/c1-5-27-17(24)18-15-9-14(21-23-11(3)19-20-16(15)23)12-7-6-10(2)13(8-12)22-28(4,25)26/h6-9,22H,5H2,1-4H3,(H,18,24) |
| InChIKey | UYBRROMMFMPJAN-UHFFFAOYSA-N |
| SMILES | CCOC(=O)NC1=CC(=NN2C1=NN=C2C)C3=CC(=C(C=C3)C)NS(=O)(=O)C |
| Reference | 1:Sci Adv. 2016 Oct 12;2(10):e1600760. eCollection 2016 Oct. Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.Picaud S,Leonards K,Lambert JP,Dovey O,Wells C,Fedorov O,Monteiro O,Fujisawa T,Wang CY,Lingard H,Tallant C,Nikbin N,Guetzoyan L,Ingham R,Ley SV,Brennan P,Muller S,Samsonova A,Gingras AC,Schwaller J,Vassiliou G,Knapp S,Filippakopoulos P, PMID: 27757418 PMCID: PMC5061470 DOI: 10.1126/sciadv.1600760 </br><span>Abstract:</span> Bromodomains (BRDs) have emerged as compelling targets for cancer therapy. The development of selective and potent BET (bromo and extra-terminal) inhibitors and their significant activity in diverse tumor models have rapidly translated into clinical studies and have motivated drug development efforts targeting non-BET BRDs. However, the complex multidomain/subunit architecture of BRD protein complexes complicates predictions of the consequences of their pharmacological targeting. To address this issue, we developed a promiscuous BRD inhibitor [bromosporine (BSP)] that broadly targets BRDs (including BETs) with nanomolar affinity, creating a tool for the identification of cellular processes and diseases where BRDs have a regulatory function. As a proof of principle, we studied the effects of BSP on leukemic cell lines known to be sensitive to BET inhibition and found, as expected, strong antiproliferative activity. Comparison of the modulation of transcriptional profiles by BSP after a short exposure to the inhibitor resulted in a BET inhibitor signature but no significant additional changes in transcription that could account for inhibition of other BRDs. Thus, nonselective targeting of BRDs identified BETs, but not other BRDs, as master regulators of context-dependent primary transcription response. |
