PARP-2/1-IN-2

Cat. No.: HY-105253: FAQs
Data Sheet Handling Instructions

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PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with K_is 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.

For research use only. We do not sell to patients.

PARP-2/1-IN-2 Chemical Structure

CAS No. : 912444-01-0

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

PARP2

2 nM (Ki)

PARP1

5 nM (Ki)

In Vivo

PARP-2/1-IN-2 (Compound 4a) (25 or 50 mg/kg; i.p.) attenuates pain in Cisplatin (HY-17394) and Oxaliplatin (HY-17371)-induced neuropathy in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Molecular Weight

244.29

Formula

C₁₃H₁₆N₄O

CAS No.

912444-01-0

SMILES

NC(C1=C2C(N=C([C@]3(C)CCCN3)N2)=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]

PARP-2/1-IN-2 Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PARP-2/1-IN-2912444-01-0PARPpoly ADP ribose polymeraseCisplatinOxaliplatinC57BL6JneuropathyVeliparibInhibitorinhibitorinhibit

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