BromosporineBromodomain inhibitor,non-selective CAS# 1619994-69-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1619994-69-2 | SDF | Download SDF |
| PubChem ID | 72943187 | Appearance | Powder |
| Formula | C17H20N6O4S | M.Wt | 404.44 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 51.7 mg/mL (127.83 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | ethyl N-[6-[3-(methanesulfonamido)-4-methylphenyl]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate | ||
| SMILES | CCOC(=O)NC1=CC(=NN2C1=NN=C2C)C3=CC(=C(C=C3)C)NS(=O)(=O)C | ||
| Standard InChIKey | UYBRROMMFMPJAN-UHFFFAOYSA-N | ||
| Standard 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Bromosporine is a non-selective inhibitor of bromodomain. | |||||
| Targets | bromodomain | |||||
Bromosporine Dilution Calculator
Bromosporine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4726 mL | 12.3628 mL | 24.7255 mL | 49.4511 mL | 61.8139 mL |
| 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | 9.8902 mL | 12.3628 mL |
| 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL | 4.9451 mL | 6.1814 mL |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4945 mL | 0.989 mL | 1.2363 mL |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.4945 mL | 0.6181 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Bromosporine is a broad spectrum inhibitor of bromodomains with IC50 value of 0.41 μM, 0.29μM, 0.122μM for BRD2, BRD4 and BRD9, respectively [1].
Bromodomains is a 110 amino acid protein domain which can recognize monoacetylated lysine residues and play a pivotal role in the targeting of chromatin-modifying enzymes to specific sites. It has been revealed that proteins contained BRDs involves in the development of many diseases, including cancers, inflammatory diseases and neurological diseases.
It is also reported that Bromosporine functioned on BAZ2A, BRPF3, CECR2, FALZ and TIF-1α with IC50 value of 9.36μM, 48.11μM, 0.017μM, 5.655μM and 12.38μM, respectively [1].
Reference:
[1]. University of Oxford. Structural Genomics Consortium Nuffield Dept. of Clinical Medicine. 15th Hellenic Symposium of Medicinal Chemistry Athens, 30, May, 2012.
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Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.[Pubmed:27757418]
Sci Adv. 2016 Oct 12;2(10):e1600760.
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.
