BGP-15

SKU: orb1303958

Description

BGP-15 2HCl is a small molecule PARP inhibitor investigated for its cytoprotective properties. Research indicates it mitigates cellular damage in models of ischemia-reperfusion injury, making it a tool for studying cardiac, neurological, and organ preservation pathways in both in vitro and in vivo experimental settings.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 66611-37-8
• MW: 351.27
• Purity: 99.99% (May vary between batches)
• Formula: C₁₄H₂₄Cl₂N₄O₂
• SMILES: Cl.Cl.N\C(=N/OCC(O)CN1CCCCC1)c1cccnc1
• Target: PARP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.69 mM);Ethanol:65 mg/mL (185.04 mM);H2O:64 mg/mL (182.2 mM);DMSO:65 mg/mL (185.04 mM)

Bioactivity

• Target IC50:
  PARP:120 μM
• In Vivo:
  BGP-15 acts as an in vitro inducer of HSP72, effective only when co-treated with heat shock, without affecting HSP90 levels. At a concentration of 200 μM, BGP-15 mitigates the depletion of high-energy phosphate compounds and prevents oxidative damage induced by imatinib mesylate. This is achieved by promoting the phosphorylation of Akt and GSK-3beta, and inhibiting the activation of p38 MAPK and JNK, thereby altering the signaling effects of imatinib mesylate. Moreover, BGP-15 significantly inhibits the activation of p38 and JNK, enzymes known to facilitate cell death and inflammatory responses in ex vivo perfused hearts.
• In Vitro:
  In two mouse models developed to exhibit heart failure and atrial fibrillation, BGP-15 has been shown to enhance cardiac function and reduce arrhythmia . Pretreatment with BGP-15 (100-200 mg/kg, p.o.) before cisplatin administration can either prevent or significantly inhibit the development of cisplatin-induced acute renal failure. BGP-15 demonstrates significant antioxidant effects on the kidneys in the context of cisplatin-induced nephrotoxicity. Despite BGP-15's ability to protect the kidneys from nephrotoxic effects, it does not diminish the antitumor efficacy of cytostatic agents. In the kidneys, BGP-15 inhibits cisplatin-induced poly(ADP-ribose) polymerization .
• Cell Research:
  Human tumor cell lines A549, HCT-15, HCT-116, and Du-145 were maintained in RPMI 1640 medium supplemented with 10% FCS in humidified air containing 5% CO2. For in vitro cytotoxicity assays, 5×103 to 5×104 cells were plated into the wells of 96-well plates in 100 μL culture medium. On the following day, cells were exposed to BGP-15 (10, 30, 100 μg/mL) and to a series of concentrations of cisplatin either by itself or in combination. Cultures were incubated in a total volume of 200 μL for 3 more days at 37°. Samples were prepared in duplicates or triplicates. Cell growth was evaluated by MTT or SRB assays. Growth inhibition curves were calculated. (Only for Reference)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PARP, BGP 15, BGP15, BGP-15, BGP-15 2HCl, BGP15 2hydrobromide, poly ADP ribose polymerase

Compound Identifiers

PubChem CID

9884807