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XZ9002 | XZ9002 : Degrader (PROTAC) of HDAC3
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
HDAC3
  • IC50:350 ± 70
  • DC50:42 nM
Degrader (PROTAC)
up to 200 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
No significant changes in the protein levels of HDACs 1, 2, and 6 were observed under the same condi ...

Potency
Cellular
In Vitro

HDAC3

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1039/D0CC03243C

Negative Control Compounds

XY9002-NC
SMILES: CCCNNC(=O)C1=CC=C(C=C1)C2=CC=C(C=C2)NC(=O)CC(=O)N[C@H](C(=O)N3C[C@H](C[C@@H]3C(=O)N[C@@H](C)C4=CC=C(C=C4)C5=C(C)N=CS5)O)C(C)(C)C

Chemical Information

Molecular Formula C47H61N7O6S
SMILEs CCCNNC(=O)c1ccc(-c2ccc(NC(=O)CCCCCCC(=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/C47H61N7O6S/c1-7-26-49-53-44(58)36-20-16-33(17-21-36)34-22-24-37(25-23-34)51-40(56)12-10-8-9-11-13-41(57)52-43(47(4,5)6)46(60)54-28-38(55)27-39(54)45(59)50-30(2)32-14-18-35(19-15-32)42-31(3)48-29-61-42/h14-25,29-30,38-39,43,49,55H,7-13,26-28H2,1-6H3,(H,50,59)(H,51,56)(H,52,57)(H,53,58)/t30-,38+,39-,43+/m0/s1
Molecular weight 851.44 Da
AlogP 0.0
HBond acceptors 13
HBond donors 6
Atoms 122

References

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Expert Reviews

by SERP
(on 20 Feb 2025 )
Cellular Use Rating
This PROTAC does not achieve a high level of HDAC3 degradation (less than 80%). However, degradation is specific for HDAC3 versus HDAC1, 2 or 6. Overall selectivity has not been assessed as proteomics...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
This PROTAC is not a selective degrader but pan-inhibitor (2-fold selectivity over HDAC1, 5-fold selectivity over HDAC2). Even though it potently degrades HDAC3, it may still have inhibitory effects on...
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