BGP-15 2HCl

Name: BGP-15 2HCl
Brand: Selleck Chemicals
SKU: S8370
Rating: 5 (0 reviews)

For research use only. Not for use in humans.

Catalog No.S8370

Molecular Weight(MW): 351.27

BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury.

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Biological Activity

Description

BGP-15, is a nicotinic amidoxime derivative with PARP inhibitory activity. It has been demonstrated that BGP-15 protects against ischemia-reperfusion injury.

Targets

PARP ^[1]

In vitro

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^[3]. 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^[4].

In vivo

BGP-15 improves cardiac function and reduces arrhythmic episodes in two independent mouse models, which progressively develop HF and AF^[2]. BGP-15 administered in 100-200 mg/kg oral doses shortly before cisplatin treatment either prevented or significantly inhibited the development of cisplatin-induced acute renal failure. BGP-15 had a significant effect on the antioxidant status of kidney during cisplatin-induced nephrotoxicity. It elevated the decreased glutathione and catalase levels, but did not affect SOD activity. BGP-15 treatment decreased the cisplatin-caused ROS production and restored the level of high energy phosphate intermediates. While BGP-15 protected against cisplatin-induced nephrotoxicity, it did not reduce the antitumor efficacy of this cytostatic agent. BGP-15 increased the survival of cisplatin-treated P-388 leukemia bearing mice. BGP-15 inhibits the cisplatin-induced poly-ADP-ribosylation in the kidney. At the same time, BGP-15 restored the cisplatin-induced disturbance in energy metabolism and preserved the ATP level in the protected tissue^[1].

Protocol

Cell Research:

^[1]

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Cell lines: Human tumor cell lines A549, HCT-15, HCT-116, and Du-145
Concentrations: 10, 30, 100 μg/mL
Incubation Time: 3 days
Method:
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)

Animal Research:

^[1]

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Animal Models: NMRI CV1 mice, BD2F1 mice and Wistar rats
Formulation: water or physiological saline
Dosages: 100, 200 mg/kg
Administration: p.o.
(Only for Reference)

References

[4] Sarszegi Z, et al. Mol Cell Biochem. 2012, 365(1-2):129-37.

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Solubility (25°C)

In vitro	DMSO	70 mg/mL (199.27 mM)
	Water	70 mg/mL (199.27 mM)
	Ethanol	70 mg/mL (199.27 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download BGP-15 2HCl SDF

Molecular Weight	351.27
Formula	C₁₄H₂₂N₄O₂.2HCl
CAS No.	66611-37-8
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	Cl.Cl.NC(=N\OCC(O)CN1CCCCC1)/C2=CC=CN=C2

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