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STM2457 | STM2457 : SAM competitive inhibitor of METTL3
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
METTL3
  • IC50:16.9 nM
  • Kd:1.4 nM
  • IC50:1520 nM
  • IC50:2810 nM
SAM competitive
up to 10 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
KinomeScan, DiscoverX
Selectivity Assessment Description:
STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases ...

Potency
Cellular
In Vitro

METTL3

Mode of Action: SAM competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41586-021-03536-w

In Vivo Validations

Mouse
Dose: 30-50 mg/Kg
Route of delivery: Intraperitoneal

DOI Reference: 10.1038/s41586-021-03536-w

Negative Control Compounds

STM2120

Chemical Information

Molecular Formula C25H28N6O2
SMILEs O=C(NCc1cn2cc(NCCC3CCCCC3)ccc2n1)c1cc(=O)n2ccccc2n1
InChI InChI=1S/C25H28N6O2/c32-24-14-21(29-23-8-4-5-13-31(23)24)25(33)27-15-20-17-30-16-19(9-10-22(30)28-20)26-12-11-18-6-2-1-3-7-18/h4-5,8-10,13-14,16-18,26H,1-3,6-7,11-12,15H2,(H,27,33)
Molecular weight 444.23 Da
AlogP 0.0
HBond acceptors 8
HBond donors 2
Atoms 61

References

Publications

Cross References

canSAR

Vendors

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Expert Reviews

by SERP
(on 20 May 2021 )
Cellular Use Rating
In Model Organisms
STM2457 is a best-in-class probe at present. I think it is great to use in cell assays since potency and binding are good and consistent with cellular thermal shift. The PK details are limited. It is...
by SERP
(on 4 Jun 2021 )
Cellular Use Rating
In Model Organisms
STM2457 is a potent and selective probe with demonstrated on target cell activity. The compound was shown to be active against leukemia cell lines and leukemia PXD models.
by SERP
(on 25 Jun 2021 )
Cellular Use Rating
In Model Organisms
Valuable first-in-class chemical probe. Robust characterization of specific target engagement is provided. Selectivity within narrow and broad enzyme families demonstrated. The compound is suitable...
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