BGP-15 (66611-37-8) Description:
BGP-15 is a novel poly(ADP-ribose) polymerase inhibitor – protects against nephrotoxicity of cisplatin without compromising its antitumor activity. BGP-15 also inhibits caspase-independent programmed cell death in acetaminophen-induced liver injury. Moreover, the hydroxylamine derivative BGP-15 is a coinducer of HSP72 in vitro, but only in the presence of cotreatment with heat and had no effect on HSP90 levels. BGP-15 (200 μM) prevented the imatinib mesylate-induced oxidative damages, attenuated the depletion of high-energy phosphates, altered the signaling effect of imatinib mesylate by preventing p38 MAP kinase and JNK activation, and induced the phosphorylation of Akt and GSK-3beta. The suppressive effect of BGP-15 on p38 and JNK activation could be significant because these kinases contribute to the cell death and inflammation in the isolated perfused heart.
The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. BGP-15 is a PARP inhibitor and insulin sensitizer. In perfused heart, it blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78, resulting in decreased levels of reactive oxygen species, lipid peroxidation, and single-strand DNA breaks. BGP-15 acts as a co-inducer of heat shock protein 72, augmenting expression induced by heat shock factor 1 in adipocytes and skeletal muscles and improving insulin sensitivity.
BGP-15 (66611-37-8) Specifications:
|Synonyms||BGP15; BGP 15; BGP15 hydrochloride; BGP15 HCl; O-(3-piperidino-2-hydroxy-1-propyl)nicotinic amidoxime|
|Chemical Name||N-(2-hydroxy-3-(piperidin-1-yl)propoxy)nicotinimidamide dihydrochloride; 3-Pyridinecarboximidamide, N-(2-hydroxy-3-
(1-piperidinyl)propoxy)-, hydrochloride (1:2).
|Molecular Weight||351.272 g/mol|
|Monoisotopic Mass||350.128 g/mol|
|Solubility||Soluble in DMSO, not in water|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||≥ 2 years|
|Handling||Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed|
|Application||BGP-15 is a PARP inhibitor, that can protect against heart failure and atrial fibrillation in mice.|