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AZ0108 | AZ0108 : NAD+ competitive inhibitor of PARP1, PARP2, PARP6
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
  • IC50:<30nM
  • EC50:53 nM
PARP2
  • IC50:<30 nM
  • EC50:53 nM
PARP6
  • IC50:83 nM
  • EC50:53 nM
NAD+ competitive
100 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PARP3 2.8 uM, TNKS 2.3 uM, TNKS2 <3 uM

Potency Assay Off-Target:
AZ0108 inhibits PARPs 1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1, a ...

Potency
Cellular
In Vitro

PARP1

Mode of Action: NAD+ competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2015.10.079

PARP2

Mode of Action: NAD+ competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2015.10.079

PARP6

Mode of Action: NAD+ competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.bmcl.2015.10.079

In Vivo Validations

Rat, mouse
Dose:
Route of delivery: Intravenous
Plasma half life: 2.3 hr (rat), 4.2 hr (mouse)
Systemic clearance: 17 mL/min•kg (rat); 15 mL/min•kg (mouse)

DOI Reference: 10.1016/j.bmcl.2015.10.079

Orthogonal Probes def

OLAPARIB
VELIPARIB
TALAZOPARIB

Chemical Information

Molecular Formula C24H20F4N6O2
SMILEs C[C@H]1Cn2c(nnc2C(C)(F)F)CN1C(=O)c1cccc(C(F)(F)c2n[nH]c(=O)c3ccccc23)c1
InChI InChI=1S/C24H20F4N6O2/c1-13-11-34-18(29-32-22(34)23(2,25)26)12-33(13)21(36)14-6-5-7-15(10-14)24(27,28)19-16-8-3-4-9-17(16)20(35)31-30-19/h3-10,13H,11-12H2,1-2H3,(H,31,35)/t13-/m0/s1
Molecular weight 500.16 Da
AlogP 3.8109
HBond acceptors 8
HBond donors 1
Atoms 56

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 12 Aug 2016 )
Cellular Use Rating
In Model Organisms
Probe use in model organism: A further publication concerning in-depth details of the biological effects was announced in the key reference paper (reference 23).
by SERP
(on 8 Sept 2016 )
Cellular Use Rating
In Model Organisms
AZ0108 potently declusters centrosomes in HeLa cells (EC50 = 53 nM) and kills a DLBCL cell line (GI50 = 17 nM). More studies are needed to determine how useful this probe is, including linking the phenotype...
by SERP
(on 8 Sept 2016 )
Cellular Use Rating
In Model Organisms
AZ0108 is also reported to have a GI50 of 0.017 uM in the DLBCL cell line OCI-LY-19. Although this compound seems promising, additional studies are needed to determine how useful it will be as a probe....
AZ0108 is a more selective PARP enzyme inhibitor (i.e., PARP 1, 2, and 6) compared with other more broad-acting PARP inhibitors. AZ0108 has cellular effects.

Portal Comments

AZ0108 is a more selective PARP enzyme inhibitor (i.e., PARP 1, 2, and 6) compared with other more broad-acting PARP inhibitors. AZ0108 has cellular effects.

(last updated: 12 Sept 2016)

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