Chemical Probes logo
MLKL Degrader 1 | MLKL Degrader 1 : Degrader (PROTAC) of MLKL
RATINGS:
Cellular Use: (3 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MLKL
  • Kd:32 nM
  • DC50:2400 ± 500 nM
  • Dmax:93%
  • EC50:1200 nM
Degrader (PROTAC)
10 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Assessment of off-target degradation of RIPK1 and/or RIPK3: no detectable binding to RIPK1 and RIPK3 ...

Potency
Cellular
In Vitro

MLKL

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c00665

Chemical Information

Molecular Formula C46H55F2N9O9S
SMILEs COc1ccc(C(=O)N2CCC3(CCN(C(=O)CCCCCCCOc4cccc(Nc5[nH]nc(-c6ccc(NS(=O)(=O)C(F)F)cc6)c5C(N)=O)c4)CC3)CC2)cc1N1CCC(=O)NC1=O
InChI InChI=1S/C46H55F2N9O9S/c1-65-36-16-13-31(28-35(36)57-22-17-37(58)51-45(57)62)43(61)56-25-20-46(21-26-56)18-23-55(24-19-46)38(59)10-5-3-2-4-6-27-66-34-9-7-8-33(29-34)50-42-39(41(49)60)40(52-53-42)30-11-14-32(15-12-30)54-67(63,64)44(47)48/h7-9,11-16,28-29,44,54H,2-6,10,17-27H2,1H3,(H2,49,60)(H2,50,52,53)(H,51,58,62)
Molecular weight 947.38 Da
AlogP 6.6028000000000056
HBond acceptors 18
HBond donors 6
Atoms 122

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 30 Oct 2024 )
Cellular Use Rating
MLKL Degrader 1 is currently the best compound available to study MLKL and its direct link to necroptosis in cells. Orthogonal compounds for investigating MLKL and necroptosis have been reported, however,...
by SERP
(on 30 Oct 2024 )
Cellular Use Rating
Selectivity profiling is required before this compound is considered for use as a probe for MLKL. It seems that rather a high concentration is required for full MLKL degradation, and at that high concentration...
by SERP
(on 2 Dec 2024 )
Cellular Use Rating
These doses are too high to be considered a useful probe compound - most degraders function at the low nM level in cells and at these doses it would not be unexpected that the probe may have off-target...
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