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IRAK3-PROTAC 23 | IRAK3-PROTAC 23 : Degrader (PROTAC) of IRAK3
RATINGS:
Cellular Use: (3 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
IRAK3
  • IC50:4.9 nM
  • DC50:2 nM
  • DC50:2 nM
Degrader (PROTAC)
100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within family: Selective against IRAK4 1400 nM and IRAK1 2300 nM. Kinome selectivity of ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selective degradation was confirmed using global proteomic profiling in THP1 cells where only IRAK3 ...

Potency
Cellular
In Vitro

IRAK3

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.0c01125

Negative Control Compounds

CANSAR3575573
Notes: PROTAC 24 is inactive in binding of CRBN

Chemical Information

Molecular Formula C47H63N11O6
SMILEs CC(C)c1ccn2ncnc(N[C@H]3CC[C@@H](N4CCN(C(=O)CCC(=O)N5CCC(CCN6CCN(c7ccc8c(c7)C(=O)N(C7CCC(=O)NC7=O)C8=O)CC6)CC5)CC4)CC3)c12
InChI InChI=1S/C47H63N11O6/c1-31(2)36-16-20-57-43(36)44(48-30-49-57)50-33-3-5-34(6-4-33)53-25-27-56(28-26-53)42(61)12-11-41(60)55-18-14-32(15-19-55)13-17-52-21-23-54(24-22-52)35-7-8-37-38(29-35)47(64)58(46(37)63)39-9-10-40(59)51-45(39)62/h7-8,16,20,29-34,39H,3-6,9-15,17-19,21-28H2,1-2H3,(H,48,49,50)(H,51,59,62)/t33-,34+,39?
Molecular weight 877.50 Da
AlogP 0.0
HBond acceptors 17
HBond donors 2
Atoms 127

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 13 Oct 2023 )
Cellular Use Rating
This compound is recommended as an in vitro tool. It has not been validated for in vivo use.
by SERP
(on 24 Dec 2023 )
Cellular Use Rating
IRAK3-PROTAC 23 is a great chemical probe for in cellulo experiments. This PROTAC exhibits very potent degradation of IRAK3 in THP1 cell line. The mechanism of acion has been well investigated. The inhibitory...
by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
IRAK3-PROTAC 23 shows potent degredation of IRAK3 in the THP1 cell line and primary macrophages. Global proteomics show selective IRAK3 degradation compared at 100 nM concentration in THP1 cells. One cell...
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