STM2457

SKU: orb1298402

Description

STM2457

Research Area

Cell Biology

Key Properties

• CAS Number: 2499663-01-1
• MW: 444.53
• Purity: 99.42%
• Formula: C₂₅H₂₈N₆O₂
• SMILES: O=C(NCc1cn2cc(CNCC3CCCCC3)ccc2n1)c1cc(=O)n2ccccc2n1
• Target: Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.22 mg/mL (4.99 mM);10% DMSO+30% PEG300+5% Tween 80+55% ddH2O:4.76 mg/mL (10.71 mM);DMSO:49.5 mg/mL (111.35 mM)

Bioactivity

• Target IC50:
  AML cells:0.6-10.3 μM|METT L3 cells:16.9 nM|MOLM-13 cells:8.699 μM
• 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. 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.
• 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, Apoptosis, autoimmune diseases, leukaemia, Inhibitor, myeloid, inhibit, METTL3, STM 2457, STM2457, STM-2457

Compound Identifiers

PubChem CID

155167581