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Niraparib | Niraparib : Inhibitor of PARP1 and PARP2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PARP1
  • IC 50:3.2 nM
  • IC 50:3.8 nM
  • IC 50:16.7 nM
  • EC 50:4 nM
PARP2
  • IC 50:2.1 nM
  • IC 50:15.3 nM
  • EC 50:4 nM
Inhibitor
Up to 50 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - TNKS 570 nM, PARP3 296 nM, PARP4 446 nM, PARP12 79 nM

Potency Assay Off-Target:
In TCA precipitation assays, MK-4827 was at least 300-fold selective for PARP1 and PARP2 over TNKS, ...
Selectivity Assessment Description:
In TCA precipitation assays, MK-4827 was at least 300-fold selective for PARP1 and PARP2 over TNKS, ...

Potency
Cellular
In Vitro

PARP1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm901188v

PARP2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm901188v

In Vivo Validations

Rat, mouse
Dose:
Route of delivery: Intravenous
Plasma half life: 3.4 hr (rat)
Systemic clearance: 28 mL/min/kg (rat)
Organ of interest (O): MDA-MB-436 xenograft
Target engagement assay: Not available

DOI Reference: 10.1021/jm901188v

Orthogonal Probes def

OLAPARIB
VELIPARIB
VELIPARIB
TALAZOPARIB

Chemical Information

Molecular Formula C19H20N4O
SMILEs NC(=O)c1cccc2cn(-c3ccc([C@@H]4CCCNC4)cc3)nc12
InChI InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1
Molecular weight 320.16 Da
AlogP 2.591400000000001
HBond acceptors 5
HBond donors 3
Atoms 44

References

Publications

Cross References

GDSC2

Vendors

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Expert Reviews

by SERP
(on 17 Aug 2016 )
Cellular Use Rating
In Model Organisms
Though this looks like a good tool compound for PARPs, due to the issues with other PARP inhibitors, it would be a good idea to use this probe side-by-side with a structurally distinct inhibitor to...
by SERP
(on 3 Jan 2017 )
Cellular Use Rating
In Model Organisms
Niraparib is a PARP 1/2 inhibitor. This agent is an excellent tool to study PARP inhibition in both the cellular and in vivo setting. However, an important study about the mechanism of these probes...
by SERP
(on 16 May 2017 )
Cellular Use Rating
In Model Organisms
The compound is reported to be a potent and selective PARP1/2 inhibitor. I have no significant concerns about recommending this compound for use as a chemical probe. In an ideal world, an inactive, closely...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria