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Homer | Homer : Degrader (PROTAC) of WDR5
RATINGS:
Cellular Use: (3 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
WDR5
  • Kd:18 nM
  • DC50:53 nM
  • Dmax:DCmax: 58% at 1 µM
Degrader (PROTAC)
Dependent on the cell line of interest, higher concentrations might be required
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Quantitative Proteomics revealed that only WDR5 is significantly and substantially depleted by Homer ...

Potency
Cellular
In Vitro

WDR5

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.1c00146

Negative Control Compounds

nc-VHL
nc-WDR5

Chemical Information

Molecular Formula C52H60F3N9O7S
SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCNC(=O)c2ccc(-c3ccc(N4CCN(C)CC4)c(NC(=O)c4c[nH]c(=O)cc4C(F)(F)F)c3)cc2)C(C)(C)C)cc1
InChI InChI=1S/C52H60F3N9O7S/c1-31-45(72-30-59-31)34-11-9-32(10-12-34)27-58-49(70)42-25-37(65)29-64(42)50(71)46(51(2,3)4)61-43(66)8-6-7-19-56-47(68)35-15-13-33(14-16-35)36-17-18-41(63-22-20-62(5)21-23-63)40(24-36)60-48(69)38-28-57-44(67)26-39(38)52(53,54)55/h9-18,24,26,28,30,37,42,46,65H,6-8,19-23,25,27,29H2,1-5H3,(H,56,68)(H,57,67)(H,58,70)(H,60,69)(H,61,66)/t37-,42+,46-/m1/s1
Molecular weight 1011.43 Da
AlogP 0.0
HBond acceptors 16
HBond donors 6
Atoms 132

Expert Reviews

by SERP
(on 14 Apr 2022)
Cellular Use Rating
I strongly encourage the usage of the available negative control compound (nc_VHL) that are incapable of binding VHL. This compound has near-identical physicochemical properties and retains any residual...
by SERP
(on 21 Apr 2022)
Cellular Use Rating
Recommended to use with both provided negative controls.
by SERP
(on 20 Feb 2025)
Cellular Use Rating
We recommend using this compound with its two negative controls, however, if a complete knockout is required, it will only result in a Dmax of 58%. In VHL-overexpressing cells, it was shown that the Dmax...
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