Chemical Probes logo
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
Download

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

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

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