Chemical Probes logo
QC-01-175 | QC-01-175 : Degrader (PROTAC) of MAPT
RATINGS:
Cellular Use: (3 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
MAPT
  • Dmax:70-80%
Degrader (PROTAC)
1 µM and 10 µM
100 nM, up to 10 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Multiplexed MS-based proteomics was employed to identify potential off-targets of the QC-01–175 degr ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
QC-01–175 was tested in an in vitro MAO assay showing high selectivity with IC50 > 8500 nM compared ...

Potency
Cellular
In Vitro

MAPT

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.7554/eLife.45457

Negative Control Compounds

QC-03-075
SMILES: O=C1NCCCC1N2C(C3=C(C(NCCOCCOCCNC(CCC4=CC5=C(C6=C(C=CN=C6)N5)C=C4)=O)=CC=C3)C2=O)=O

Chemical Information

Molecular Formula C33H34N6O7
SMILEs O=C(CCc1ccc2c(c1)[nH]c1ccncc12)NCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
InChI InChI=1S/C33H34N6O7/c40-28(8-5-20-4-6-21-23-19-34-11-10-24(23)37-26(21)18-20)36-13-15-46-17-16-45-14-12-35-25-3-1-2-22-30(25)33(44)39(32(22)43)27-7-9-29(41)38-31(27)42/h1-4,6,10-11,18-19,27,35,37H,5,7-9,12-17H2,(H,36,40)(H,38,41,42)
Molecular weight 626.25 Da
AlogP 2.3114
HBond acceptors 13
HBond donors 4
Atoms 80

References

Publications

Cross References

canSARChEMBL

Vendors

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

Expert Reviews

by SERP
(on 19 Aug 2023 )
Cellular Use Rating
QC-01-175 is not a potent tau degrader, but it is well validated, so this compound is one of the good options to evaluate the biological effect of eliminating mutant tau from neurons.
by SERP
(on 27 Aug 2023 )
Cellular Use Rating
QC-01-175 can be considered as a pathfinder probe for tau degradation. For example this compound can be used for assay validation purposes. However, its lack of selectivity precludes use for cell biology...
by SERP
(on 8 Sept 2023 )
Cellular Use Rating
Considering that MS-based proteomic profiling of QC-01-175 in A152T neurons was conducted at a concentration of 1 uM, it is important to note that the selectivity of this probe at 10 uM remains unknown....
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