Bromosporine --- Pan-bromodomain Inhibitor

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.

Product information

CAS Number: 1619994-69-2

Molecular Weight: 404.44

Formula: C17H20N6O4S

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

Smiles: CC1=NN=C2C(=CC(=NN12)C1=CC=C(C)C(=C1)NS(C)(=O)=O)NC(=O)OCC

InChiKey: UYBRROMMFMPJAN-UHFFFAOYSA-N

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)

Technical Data

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

In Vitro:

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.

In Vivo:

n/a

References:

1. 15th HELLENIC SYMPOSIUM OF MEDICINAL CHEMISTRY.
2. 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.

Products are for research use only. Not for human use.

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