PARP-2/1-IN-2

PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity[1].

Signaling Pathways >> Epigenetics >> PARP

Research Areas >> Neurological Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

PARP2:2 nM (Ki)

PARP1:5 nM (Ki)

PARP-2/1-IN-2 (Compound 4a) (25 or 50 mg/kg; i.p.) 在 Cisplatin (HY-17394) 和 Oxaliplatin (HY-17371) 诱导的小鼠神经病变中减轻疼痛[1]。 Animal Model: Male C57BL6J mice, Cisplatin (HY-17394) and Oxaliplatin (HY-17371)-induced painful neuropathy models[1] Dosage: 25 mg/kg or 50 mg/kg Administration: Intraperitoneal injection, two days prior to treatment with Cisplatin or oxaliplatin, with administration continuing by i.p. injection along with the Cisplatin or oxaliplatin regimen (5 days, followed by 5 days of rest, for two weekly cycles) Result: Does not attenuate Cisplatin and Oxaliplatin-induced body weight loss. Does not Affect the decline in exploratory behavior associated with Cisplatin and Oxaliplatin Treatment. Attenuates mechanical allodynia in Cisplatin and Oxaliplatin-induced neuropathy. Attenuates thermal hyperalgesia in Cisplatin-induced neuropathy. Attenuates cold hyperalgesia associated with Oxaliplatin-induced neuropathy.

[1]. Ta LE, et al. A novel and selective poly (ADP-ribose) polymerase inhibitor ameliorates chemotherapy-induced painful neuropathy. PLoS One. 2013;8(1):e54161.