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PARP&Proteasome

BGP-15 (66611-37-8)

BGP-15 is a novel poly(ADP-ribose) polymerase inhibitor, with roles in DNA repair and apoptosis…

Not Intended for Therapeutic Use. For research use only.

CAS: 66611-37-8 Category

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:

Product Name BGP-15
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).

Purity ≥98%
CAS Number 66611-37-8
Molecular Formula C14H24Cl2N4O2
Molecular Weight 351.272 g/mol
Monoisotopic Mass 350.128 g/mol
MDL number MFCD21603901
InChIKey ISGGVCWFTPTHIX-UHFFFAOYSA-N
InChi Code InChI=1S/C14H22N4O2.2ClH/c15-14(12-5-4-6-16-9-12)17-20-11-13(19)10-18-7-2-1-3-8-18;;/h4-6,9,13,19H,1-3,7-8,10-11H2,(H2,15,17);2*1H
SMILES N=C(NOCC(O)CN1CCCCC1)C2=CN=CC=C2.[H]Cl.[H]Cl
Form Powder
Color N/A
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.

 


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RIDADR NONH for all modes of transport

References:

  • Literati-Nagy Z, Tory K, Literáti-Nagy B, Bajza A, Vígh L Jr, Vígh L, Mandl J, Szilvássy Z. Synergic insulin sensitizing effect of rimonabant and BGP-15 in Zucker-obese rats. Pathol Oncol Res. 2013 Jul;19(3):571-5. doi: 10.1007/s12253-013-9620-6. Epub 2013 May 3. PubMed PMID: 23640247.
  • Sumegi K, Fekete K, Antus C, Debreceni B, Hocsak E, Gallyas F Jr, Sumegi B, Szabo A. BGP-15 Protects against Oxidative Stress- or Lipopolysaccharide-Induced Mitochondrial Destabilization and Reduces Mitochondrial Production of Reactive Oxygen Species. PLoS One. 2017 Jan 3;12(1):e0169372. doi: 10.1371/journal.pone.0169372. eCollection 2017. PMID: 28046125.
  • Racz I, Tory K, Gallyas F Jr, Berente Z, Osz E, Jaszlits L, Bernath S, Sumegi B, Rabloczky G, Literati-Nagy P. BGP-15 – a novel poly(ADP-ribose) polymerase inhibitor – protects against nephrotoxicity of cisplatin without compromising its antitumor activity. Biochem Pharmacol. 2002 Mar 15;63(6):1099-111. PMID: 11931842.
  • Sarszegi Z, Bognar E, Gaszner B, Kónyi A, Gallyas F Jr, Sumegi B, Berente Z. BGP-15, a PARP-inhibitor, prevents imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases. Mol Cell Biochem. 2012 Jun;365(1-2):129-37. doi: 10.1007/s11010-012-1252-8. Epub 2012 Feb 14. PubMed PMID: 22350755.
  • Berkovich L, Sintov AC, Ben-Shabat S. Inhibition of cancer growth and induction of apoptosis by BGP-13 and BGP-15, new calcipotriene-derived vitamin D3 analogs, in-vitro and in-vivo studies. Invest New Drugs. 2013 Apr;31(2):247-55. doi: 10.1007/s10637-012-9839-1. Epub 2012 Jun 2. Erratum in: Invest New Drugs. 2013 Apr;31(2):490. PubMed PMID: 22661288.