912444-01-0

912444-01-0 structure

Name: PARP-2/1-IN-2
Chemical Name: 2-[(2S)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide hydrochloride (1:2)
CAS Number: 912444-01-0
Molecular Formula: C₁₃H₂₄N₄O
Molecular Weight: 252.356
Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
Create Date: 2019-01-19 10:55:29
Modify Date: 2025-08-20 17:27:33
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].

Name	2-[(2S)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide hydrochloride (1:2)
Synonyms	1H-Benzimidazole-4-carboxamide, octahydro-2-(2-methyl-2-pyrrolidinyl)- 2-(2-Methyl-2-pyrrolidinyl)octahydro-1H-benzimidazole-4-carboxamide

Description	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].
Related Catalog	Signaling Pathways >> Epigenetics >> PARP Research Areas >> Neurological Disease Signaling Pathways >> Cell Cycle/DNA Damage >> PARP
Target	PARP2:2 nM (Ki) PARP1:5 nM (Ki)
In Vivo	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.
References	[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.

Density	1.1±0.1 g/cm3
Boiling Point	466.4±45.0 °C at 760 mmHg
Molecular Formula	C₁₃H₂₄N₄O
Molecular Weight	252.356
Flash Point	235.9±28.7 °C
Exact Mass	252.195007
LogP	-0.88
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.522

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