STM2457 (DC53045) chemical structure
Chemical structureResearch use only
CAT. NO. DC53045Featured

STM2457

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Product overview

Description & Application

STM2457 is a catalytic METTL3 inhibitor for RNA methylation, leukemia-cell differentiation and cancer research.

ParameterValue
Chemical NameSTM2457
CAS No.2499663-01-1
SynonymsSTM2457; STM-2457; STM 2457
FormulaC25H28N6O2
M.Wt444.23
SMILESC1=CC=CC2=NC(C(=O)NCC3N=C4C=CC(CNCC5CCCCC5)=CN4C=3)=CC(=O)N12
Purity>99%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
METTL3 / m6A RNA methylation · Literature evidence

Biological Activity

STM2457 is a catalytic METTL3 inhibitor for RNA methylation, leukemia-cell differentiation and cancer research. STM2457 IC50 was 16.9 nM. This enzymatic measurement should not be used as a cellular growth IC50.

In Vitro

EndpointModel / conditions / sourceReported result
Biochemical potencyMETTL3/METTL14 methyltransferase assay. [1], Fig. 1STM2457 IC50 was 16.9 nM. This enzymatic measurement should not be used as a cellular growth IC50.
AML cell phenotypeAcute myeloid leukemia models. [1]Reduced growth was accompanied by increased differentiation and apoptosis.
RNA and translationLeukemia-associated mRNA methylation and protein-expression assays. [1]Selective reductions in m6A on oncogenic transcripts were accompanied by lower protein expression consistent with impaired translation.

In Vivo

EndpointModel / conditions / sourceReported result
In-vivo responseMultiple AML mouse models. [1]STM2457 impaired leukemia engraftment and prolonged survival, including effects on key leukemia stem-cell populations.

Compound and Evidence Context

EndpointModel / conditions / sourceReported result
Study coverageCatalytic inhibition and leukemia models. [1]The evidence does not establish comparable potency in all tumors; cellular exposure and animal schedules must be interpreted separately.

Interpretation

The biochemical IC50 is not a cellular viability value; the study does not establish efficacy across every cancer type.

Original studies

Original study and figures ↗

References

  1. Yankova E, et al. Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia. Nature (2021).

Product documentation

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Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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