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dWIZ1 | dWIZ1 : Molecular Glue of WIZ
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
WIZ
  • Kd:3500 nM
  • IC50:170 nM
  • EC50:13 nM
  • Dmax:78%
  • DC50:13 nM
  • EC50:547 nM
Molecular Glue
1 µM
up to 10 µM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Primary human erythroblasts were treated with 10 μM compound C or dimethyl sulfoxide (DMSO) control ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
IKZF1 HiBiT degradation (DC50 / Dmax) >50000 nM / 0 % GSPT1 HiBiT degradation (DC50 / Dmax) >50000 n ...

Potency
Cellular
In Vitro

WIZ

Mode of Action: Molecular Glue

Structure-Activity-Relationship data available? No

DOI Reference: 10.1126/science.adk6129

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.85 h
Systemic clearance: 27.6 mL/min/Kg
Area Under the Curve:: 1440 nmol*h/L

DOI Reference: 10.1126/science.adk6129

Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 24 nM
Area Under the Curve:: 115 nmol*h/L
Bioavailability: 2.7%

DOI Reference: 10.1126/science.adk6129

Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 242 nM
Area Under the Curve:: 1120 nmol*h/L
Bioavailability: 2.7%

DOI Reference: 10.1126/science.adk6129

Chemical Information

Molecular Formula C22H29N3O4
SMILEs CCN1CCCC[C@H]1[C@H](C)Oc1ccc2c(c1)CN(C1CCC(=O)NC1=O)C2=O
InChI InChI=1S/C22H29N3O4/c1-3-24-11-5-4-6-18(24)14(2)29-16-7-8-17-15(12-16)13-25(22(17)28)19-9-10-20(26)23-21(19)27/h7-8,12,14,18-19H,3-6,9-11,13H2,1-2H3,(H,23,26,27)/t14-,18-,19?/m0/s1
Molecular weight 399.22 Da
AlogP 2.0892999999999997
HBond acceptors 7
HBond donors 1
Atoms 58

References

Publications

Cross References

Expert Reviews

by SERP
(on 15 Aug 2024 )
Cellular Use Rating
In Model Organisms
dWIZ1 is a very well characterized probe for the selective degradation of the transcription factor WIZ for in vitro assays (including primary erythroblasts) up to 10 uM (higher concentration should be...
by SERP
(on 25 Nov 2024 )
Cellular Use Rating
In Model Organisms
I recommend 1 micromolar as the single-point dosage. (I would note that proteomics was done at 10 uM and WIZ is reduced the most and with the highest significance.) The authors do not appear to indicate...
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