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KH12 | KH12 : Degrader (PROTAC) of METTL3
RATINGS:
Cellular Use: (1 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
METTL3
  • IC50:341 nM
  • DC50:220 nM
  • IC50:1040 nM
Degrader (PROTAC)
1 uM

Selectivity

Potency
Cellular
In Vitro

METTL3

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ejmech.2024.116843

Negative Control Compounds

canSAR7437535
Notes: KH12-NC is not able to reduce METTL3 levels on MOLM-13 cells.

Chemical Information

Molecular Formula C56H77F2N11O5S
SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCCCCCNc2cc(N3CCC4(CC3)CN(c3cc(F)c(CN5CCC(C)(C)CC5)cc3F)CC(=O)N4)ncn2)C(C)(C)C)cc1
InChI InChI=1S/C56H77F2N11O5S/c1-37-50(75-36-63-37)39-15-13-38(14-16-39)30-60-52(73)45-27-41(70)32-69(45)53(74)51(54(2,3)4)64-48(71)12-10-8-7-9-11-21-59-46-29-47(62-35-61-46)67-24-19-56(20-25-67)34-68(33-49(72)65-56)44-28-42(57)40(26-43(44)58)31-66-22-17-55(5,6)18-23-66/h13-16,26,28-29,35-36,41,45,51,70H,7-12,17-25,27,30-34H2,1-6H3,(H,60,73)(H,64,71)(H,65,72)(H,59,61,62)/t41-,45+,51-/m1/s1
Molecular weight 1053.58 Da
AlogP 7.345720000000007
HBond acceptors 16
HBond donors 5
Atoms 152
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

Expert Reviews

by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
While KH12 has been shown to be a potent degrader of METTL3, there is no indication of degradation selectivity in cells by proteomic studies
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