STM2457

Catalog No.S9870 Batch:S987008

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Technical Data

Formula

C25H28N6O2
Molecular Weight 444.53 CAS No. 2499663-01-1
Solubility (25°C)* In vitro DMSO 22 mg/mL (49.49 mM)
Ethanol 22 mg/mL (49.49 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% corn oil
0.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
1.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description STM2457 is a highly potent and selective first-in-class catalytic inhibitor of RNA Methyltransferase METTL3 with an IC50 of 16.9 nM. STM2457 is highly specific for METTL3 and showed no inhibition of other RNA methyltransferases.
Targets
METTL3 [1]
(Cell-free assay)
16.9 nM
In vitro

STM2457 has a highly efficient and selective catalytic inhibition on RNA methyltransferase METTL3, causing gene-expression defects consistent with an effect on the mRNA translational efficiency of m6A substrates.[1]
In vivo

STM2457 prevents acute myeloid leukaemia (AML) expansion and reduces the number of key leukaemia stem cells in vivo.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MOLM-13 cells

  • Concentrations

    0.1, 1, 5 and 10 μM

  • Incubation Time

    --

  • Method

    Western blot analysis
Animal Study:

[1]
  • Animal Models

    AML PDX-1 mice (NPM1c cells), AML PDX-2 mice (MLL-AF6 cells), AML PDX-3 mice (MLL-AF10)

  • Dosages

    50 mg/kg

  • Administration

    --

Selleck's STM2457 has been cited by 8 publications

Suppression of the METTL3-m6A-integrin β1 axis by extracellular acidification impairs T cell infiltration and antitumor activity [ Cell Rep, 2024, 43(2):113796] PubMed: 38367240
M6A-modified circRBM33 promotes prostate cancer progression via PDHA1-mediated mitochondrial respiration regulation and presents a potential target for ARSI therapy [ Int J Biol Sci, 2023, 19(5):1543-1563] PubMed: 37056926
METTL3-mediated m6A modification of IGFBP7-OT promotes osteoarthritis progression by regulating the DNMT1/DNMT3a-IGFBP7 axis [ Cell Rep, 2023, 42(6):112589] PubMed: 37270777
m6A methyltransferase METTL3 programs CD4+ T-cell activation and effector T-cell differentiation in systemic lupus erythematosus [ Mol Med, 2023, 29(1):46] PubMed: 37013484
METTL3 exacerbates insulin resistance in hepatocytes by regulating m6A modification of cytochrome P450 2B6 [ Nutr Metab (Lond), 2023, 20(1):40] PubMed: 37710320
N6-methyladenosine modification governs liver glycogenesis by stabilizing the glycogen synthase 2 mRNA [ Nat Commun, 2022, 13(1):7038] PubMed: 36396934
METTL3 overexpression aggravates LPS-induced cellular inflammation in mouse intestinal epithelial cells and DSS-induced IBD in mice [ Cell Death Discov, 2022, 8(1):62] PubMed: 35165276
METTL3 inhibition reduces N6 -methyladenosine levels and prevents allogeneic CD4+ T-cell responses [ Immunol Cell Biol, 2022, 100(9):718-730] PubMed: 36005900

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.