A4186-10mg | Bromosporine [1619994-69-2] Clinisciences

Background

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.

Product Citation

1. Alonso, Victoria Lucia, et al. "Overexpression of bromodomain factor 3 in Trypanosoma cruzi (TcBDF3) affects differentiation of the parasite and protects it against bromodomain inhibitors." FEBS Journal (2016). PMID:27007774

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	404.44
Cas No.	1619994-69-2
Formula	C₁₇H₂₀N₆O₄S
Solubility	≥40.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name	ethyl (3-methyl-6-(4-methyl-3-(methylsulfonamido)phenyl)-[1,2,4]triazolo[4,3-b]pyridazin-8-yl)carbamate
SDF	Download SDF
Canonical SMILES	CC1=C(NS(C)(=O)=O)C=C(C2=NN3C(C(NC(OCC)=O)=C2)=NN=C3C)C=C1
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.