Description
BRL-50481 (433695-36-4) is a potent and selective inhibitor of phosphodiesterase-7 (PDE7), Ki=180 nM.1Induces apoptosis in chronic lymphocytic leukemia cells which express PDE7B.2BRL-50481 increases mineralization in osteoblasts differentiated from hMSC.3Cell permeable.
Chemical Properties
Off-White Solid
Uses
A PDE7 inhibitor that has acceptable selectivity for in vivo studies
Definition
ChEBI: BRL-50481 is a C-nitro compound that is benzene substituted by N,N-dimethylaminosulfonyl, methyl and nitro groups at positions 1, 2 and 5, respectively. It is a phosphodiesterase inhibitor selective for the PDE7 subtype (Ki = 180 nM). It has a role as an EC 3.1.4.53 (3',5'-cyclic-AMP phosphodiesterase) inhibitor, a geroprotector and a bone density conservation agent. It is a sulfonamide, a C-nitro compound and a member of toluenes.
Biological Activity
Selective, substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (K i = 180 nM). Displays > 200-fold selectivity over PDE1B, PDE1C, PDE2, PDE3, PDE4A4 and PDE5.
Biochem/physiol Actions
BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).
References
[1] SUSAN J SMITH. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes.[J]. Molecular Pharmacology, 2004, 66 6: 1679-1689. DOI:
10.1124/mol.104.002246[2] LINGZHI ZHANG. Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic leukemia.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2008: 19532-19537. DOI:
10.1073/pnas.0806152105[3] MINNA PEKKINEN . Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts[J]. Bone, 2008, 43 1: Pages 84-91. DOI:
10.1016/j.bone.2008.02.021
