Chemical Probes logo
YX862 | YX862 : Degrader (PROTAC) of HDAC8
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
HDAC8
  • IC50:194.7 ± 17.1 nM
  • Activity:~ 500 nM
  • Dmax:>95%
  • IC50:720 nM
  • DC50:1.8 nM
Degrader (PROTAC)
up to 250 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
No HDAC1, 2 or 3 were observed up to 4 uM and 24h incubation.
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteome-wide target specificity of YX862 was performed using a tandem mass tag (TMT)-based quantita ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
inhibited HDAC3 with IC50 of 2330 nM

Potency
Cellular
In Vitro

HDAC8

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.4c00761

Negative Control Compounds

canSAR7385591
Notes: In cells treated with 200 nM YX862-NC, no degradation of HDAC8 was detected.

Orthogonal Probes def

GKW

Chemical Information

Molecular Formula C48H72N8O5S
SMILEs CCCCCCNNC(=O)c1ccc(N2CCN(CCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)(C)C)CC2)cc1
InChI InChI=1S/C48H72N8O5S/c1-7-8-9-14-25-50-53-45(59)38-21-23-39(24-22-38)55-29-27-54(28-30-55)26-15-12-10-11-13-16-42(58)52-44(48(4,5)6)47(61)56-32-40(57)31-41(56)46(60)51-34(2)36-17-19-37(20-18-36)43-35(3)49-33-62-43/h17-24,33-34,40-41,44,50,57H,7-16,25-32H2,1-6H3,(H,51,60)(H,52,58)(H,53,59)/t34-,40+,41-,44+/m0/s1
Molecular weight 872.53 Da
AlogP 6.7659200000000075
HBond acceptors 13
HBond donors 5
Atoms 134

References

Publications

Cross References

canSARChEMBL

Expert Reviews

by SERP
(on 20 Feb 2025 )
Cellular Use Rating
This is a potent and selective PROTAC for HDAC8 that can be used to assess the effect of HDAC8 degradation in tissue culture. It is remarkable in displaying hardly any "Hook effect".
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
This is a very potent and selective PROTAC for HDAC8 with a DC50 of 1.8 nM and Dmax > 95% in MCF7 cells. It is selective over the close family member HDAC3 at 250 nM. Proteomics confirms the compound...
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