Chemical Probes logo
RTx-161 | RTx-161 : Allosteric Inhibitor of POLQ
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
POLQ
  • IC50:4.1 nM
  • IC50:~1000 nM
  • IC50:~1000 nM
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selective against other 6 Polymerases.

Potency
Cellular
In Vitro

POLQ

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41467-024-46593-1

Orthogonal Probes def

K8I

Chemical Information

Molecular Formula C21H18F7N3O4
SMILEs CN(C(=O)Oc1c(N2CCN(CCO)C2=O)cc(C(F)(F)F)cc1C(F)(F)F)c1ccc(F)cc1
InChI InChI=1S/C21H18F7N3O4/c1-29(14-4-2-13(22)3-5-14)19(34)35-17-15(21(26,27)28)10-12(20(23,24)25)11-16(17)31-7-6-30(8-9-32)18(31)33/h2-5,10-11,32H,6-9H2,1H3
Molecular weight 509.12 Da
AlogP 4.732800000000004
HBond acceptors 7
HBond donors 1
Atoms 53

References

Publications

Cross References

Vendors

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

Expert Reviews

by SERP
(on 12 Jun 2024 )
Cellular Use Rating
RTx-161 is an inhibitor of Polθ polymerase activity that exhibits biochemical IC50 of ~4nM. Thus, this compound could be used in biochemical and biophysical studies. In terms of the data supporting its...
by SERP
(on 14 Jun 2024 )
Cellular Use Rating
The compound is potent and on-target activity is well demonstrated but selectivity profiling is quite limited and a negative control is missing.
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