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Bromosporine
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Bromosporine图片
CAS NO:1619994-69-2
规格:≥98%
包装与价格：
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
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

实验参考方法
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.

In Vivo
Animal model
Formulation & Dosage
References 15th HELLENIC SYMPOSIUM OF MEDICINAL CHEMISTRY.