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TO-1187 | TO-1187 : Degrader (PROTAC) of HDAC6
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
HDAC6
  • IC50:4.6 nM
  • DC50:5.81 nM
  • Activity:1 µM
Degrader (PROTAC)
100 nM up to 1 µM; Hook effect at 10 µM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Cellular concentrations of three HDAC isoforms (HDACs 3, 6, and 8) in human multiple myeloma cell li ...
Selectivity Assessment Description:
Nearly complete degradation of HDAC6 was observed at a single concentration of 1 μM, and no signific ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Global Degradation Proteomic Analysis of TO-1187: MM.1S cells were exposed to two different concentr ...
Selectivity Assessment Description:
At a concentration of 100 nM, TO-1187 exhibited a distinct degradation pattern. Specifically, TO-118 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Immunoblotting for IKZF1, IKZF3, and GSPT1 in MM.1S cells 6 h after treatment with 100 nM TO-1187 sh ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
In vitro inhibitory activity against four HDACs (HDACs 3, 6, 8, and 11) was assessed using an electr ...

Potency
Cellular
In Vitro

HDAC6

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.4c02021

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intravenous

DOI Reference: 10.1021/acs.jmedchem.4c02021

Chemical Information

Coming Soon...

References

Publications

Cross References

Expert Reviews

by SERP
(on 13 Jan 2026 )
Cellular Use Rating
In Model Organisms
Solid characterization of TO-1187 as degrader for HDAC6 in cell lines, but lower degradation efficiency in vivo.
by SERP
(on 10 Feb 2026 )
Cellular Use Rating
In Model Organisms
TO-1187 is highly recommended to treat human cells. More data are needed for its broad use across model organisms. For example, the selectivity of TO-1187 was only rigorously examined in the context of...
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