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Key Documents

SML3360

Sigma-Aldrich

STM2457

≥98% (HPLC)

Synonym(s):

N-[(6-{[(Cyclohexylmethyl)amino]methyl}imidazo[1,2-a]pyridin-2-yl)methyl]-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxamide, STM 2457, STM-2457

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About This Item

Empirical Formula (Hill Notation):
C25H28N6O2
CAS Number:
Molecular Weight:
444.53
UNSPSC Code:
12352200
NACRES:
NA.21

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

O=C1C=C(C(NCC2=CN3C=C(CNCC4CCCCC4)C=CC3=N2)=O)N=C5C=CC=CN15

Biochem/physiol Actions

STM2457 is a potent and highly selective SAM-binding site METTL3 (MT-A70) m6A methyltransferase inhibitor (IC50 = 16.9 nM, Kd = 1.4 nM by SPR, using METTL3-METTL14 complex; no potency toward other RNA/DNA/protein methyltransferases or 486 kinases). STM2457 selectively inhibits human AML proliferation (IC50 = 0.6-10.3 µM) and the clonogenic potential of primary mouse AML, but not normal mouse haematopoietic stem/progenitor or human cord blood CD34+ cells. STM2457 impairs the expansion of AML patient-derived xenografts in mice in vivo (50 mg/kg i.p.) and significantly prolongs the animal′s lifespan. STM2457 is also reported to restrict β-coronavirus replication and spread.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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Nadine Körtel et al.
Nucleic acids research, 49(16), e92-e92 (2021-06-23)
N6-methyladenosine (m6A) is the most abundant internal RNA modification in eukaryotic mRNAs and influences many aspects of RNA processing. miCLIP (m6A individual-nucleotide resolution UV crosslinking and immunoprecipitation) is an antibody-based approach to map m6A sites with single-nucleotide resolution. However, due
Hannah M Burgess et al.
Genes & development, 35(13-14), 1005-1019 (2021-06-26)
N6-methyladenosine (m6A) is an abundant internal RNA modification, influencing transcript fate and function in uninfected and virus-infected cells. Installation of m6A by the nuclear RNA methyltransferase METTL3 occurs cotranscriptionally; however, the genomes of some cytoplasmic RNA viruses are also m6A-modified.

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