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    Bromosporine
    Bromosporine

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0418
    CAS #: 1619994-69-2Purity ≥98%

    Description: Bromosporine is a novel, potent and broad spectrum inhibitor against BET bromodomains with potential use as a chemical probe for bromodomain functional assays. It inhibits BRD2, BRD4, BRD9 and CECR2 with IC50s of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM, respectively. Bromodomains (BRDs) are protein interaction modules that read epigenetic marks recognizing ε-N-lysine acetylation motifs. 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.

    References: http://www.thesgc.org/chemical-probes/bromosporine

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    Molecular Weight (MW)404.44
    FormulaC17H20N6O4S
    CAS No.1619994-69-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 81 mg/mL (200.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=C(OCC)NC1=CC(C2=CC=C(C)C(NS(=O)(C)=O)=C2)=NN3C1=NN=C3C
    Synonyms

    Synonym: Bromosporine

    Ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate

    InChi Key: UYBRROMMFMPJAN-UHFFFAOYSA-N

    InChi Code: 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)

    SMILES Code: O=C(OCC)NC1=CC(C2=CC=C(C)C(NS(=O)(C)=O)=C2)=NN3C1=NN=C3C 


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: 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).  


    Cell Assay: 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.

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    References 15th HELLENIC SYMPOSIUM OF MEDICINAL CHEMISTRY.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Bromosporine

    Bromosporine

    Bromosporine

    https://www.thesgc.org/chemical-probes/bromosporine


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