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DKY709 | DKY709 : Molecular glue degrader of IKZF2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
IKZF2
  • IC50:130 nM
  • Kd:190 nM
  • DC50:4 nM
  • IC50:73 nM
  • DC50:11 nM
Molecular glue
up to 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: DC50 - 13 nM (88% Dmax)

Potency Assay Off-Target:
Selective against IKZF1, GSPT1 possible SALL4 off-target was discarded after cellular assay.
In Cell Selectivity Assessment
Potency Assay Off-Target:
Quantitative proteomics profiling of Jurkat cells treated for 16 h with 2.5 μM DKY709 or DMSO displa ...

Potency
Cellular
In Vitro

IKZF2

Mode of Action: Molecular glue

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2023.02.005

In Vivo Validations

Mouse
Dose: 2 mg/Kg
Route of delivery: Intravenous
Plasma half life: 2.8 h
Systemic clearance: 18 mL/min/Kg
Volume of Distribution at Steady-State: 1.9 L/Kg

DOI Reference: 10.1016/j.chembiol.2023.02.005

Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 482 ng/mL
Tmax: 1 h
Area Under the Curve:: 1506 ng/mL*h
Bioavailability: 53%

DOI Reference: 10.1016/j.chembiol.2023.02.005

Monkey (Cynomolgus)
Dose: 0.3 mg/Kg
Route of delivery: Intravenous
Plasma half life: 5.7 h
Systemic clearance: 26 mL/min/Kg
Volume of Distribution at Steady-State: 8.6 L/Kg

DOI Reference: 10.1016/j.chembiol.2023.02.005

Dose: 1.0 mg/Kg
Route of delivery: Oral
Cmax: 41 ng/mL
Tmax: 4 h
Area Under the Curve:: 516 ng/mL*h
Bioavailability: 89%

DOI Reference: 10.1016/j.chembiol.2023.02.005

Chemical Information

Molecular Formula C25H27N3O3
SMILEs O=C1CCC(N2Cc3cc(C4CCN(Cc5ccccc5)CC4)ccc3C2=O)C(=O)N1
InChI InChI=1S/C25H27N3O3/c29-23-9-8-22(24(30)26-23)28-16-20-14-19(6-7-21(20)25(28)31)18-10-12-27(13-11-18)15-17-4-2-1-3-5-17/h1-7,14,18,22H,8-13,15-16H2,(H,26,29,30)
Molecular weight 417.21 Da
AlogP 0.0
HBond acceptors 6
HBond donors 1
Atoms 58

References

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Expert Reviews

by SERP
(on 8 Feb 2024 )
Cellular Use Rating
In Model Organisms
DKY709 is a very well-characterized molecular glue degrader of IKZF2 and an excellent probe. Similar in structure to pomalidomide, DKY709 was successfully designed to not degrade other neosubstrates of...
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