| Name | STM2457 |
| Description | STM2457 is an inhibitor of the RNA methyltransferase METTL3 (IC50=16.9 nM) with selective and oral activity.STM2457 can be used in acute myeloid leukemia (AML) studies. |
| In vitro | METHODS: Eight human acute myeloid leukemia cells AML were treated with STM2457 (0-100 μM) for 72 h. Cell proliferation was detected using CellTiter 96 AQueous Non-Radioactive Cell Proliferation Assay.
RESULTS: STM2457-treated AML cell lines showed a significant reduction in growth after treatment in a concentration-dependent manner, with IC50s ranging from 0.6-10.3 μM. [1]
METHODS: Human lung cancer cells A549 and H1975 were treated with STM2457 (1-5 μM) for 3-6 days and apoptosis was detected using Flow Cytometry.
RESULTS: STM2457 induced apoptosis in A549 and H1975 cells. [2] |
| In vivo | METHODS: To assay anti-tumor activity in vivo, STM2457 (50 mg/kg) was administered intraperitoneally to NSG mice bearing xenografts derived from human AML patients once daily for twelve to fourteen days.
RESULTS: Daily treatment with STM2457 resulted in impaired implantation and AML amplification in vivo and significantly prolonged mouse lifespan. [1]
METHODS: To investigate the role of METTL3 in the pathogenesis of systemic lupus erythematosus (SLE), STM2457 (30 mg/kg) was administered intraperitoneally to a cGVHD lupus mouse model once every three days for ten weeks.
RESULTS: METTL3 inhibition increased antibody production and exacerbated the lupus-like phenotype in cGVHD mice.METTL3 inhibition is involved in the pathogenesis of SLE by participating in the imbalance between CD4+ T cell activation and effector T cell differentiation. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 49.5 mg/mL (111.35 mM), Sonication and heating are recommended.
10% DMSO+30% PEG300+5% Tween 80+55% ddH2O : 4.76 mg/mL (10.71 mM), Solution.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.22 mg/mL (4.99 mM), Solution.
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| Keywords | STM-2457 | STM2457 | STM 2457 | myeloid | METTL3 | leukaemia | Inhibitor | inhibit | cancer | autoimmune diseases | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | Bioactive Compound Library | Hematonosis Compound Library | Anti-Viral Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
