FB23-2

SKU: orb1300035

Description

FB23-2 is a potent and selective small molecule inhibitor of the m6A demethylase FTO, exhibiting an IC50 of 2.6 µM. It serves as a valuable chemical probe for investigating the role of m6A modification in areas such as cancer, obesity, and neurological disorders in both cellular and animal models.

Research Area

Cell Biology

Key Properties

• CAS Number: 2243736-45-8
• MW: 392.2
• Purity: >98%
• Formula: C₁₈H₁₅Cl₂N₃O₃
• SMILES: Cc1noc(C)c1-c1cc(Cl)c(Nc2ccccc2C(=O)NO)c(Cl)c1
• Target: Nucleic acid methylation
• Solubility: Soluble in DMSO (up to at least 20 mg/ml)

Bioactivity

• Target IC50:
  FTO:2.6 μM (IC50)
• In Vivo:
  FB23-2 significantly inhibits the progression of human AML cell lines and primary cells in xeno-transplanted mice.
• In Vitro:
  FB23-2 directly bind to FTO and selectively inhibit FTO's m6A demethylase activity. Mimicking FTO depletion, FB23-2 dramatically suppresses proliferation and promotes the differentiation/apoptosis of human acute myeloid leukemia (AML) cell line cells and primary blast AML cells in vitro.
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• Cell Research:
  Quantitation of FB23 and FB23-2 in AML cells: NB4 and MONOMAC6 cells were treated with 10 μM FB23 or FB23-2 for 24 hr, respectively. Viable cells were distinguished with 0.1% trypan blue, counted and then harvested with PBS by several washings. Cells were diluted into 100 μl with 50% (v/v) water/methanol and followed by several shock freeze-thaw cycles. The supernatants were collected for analysis. The Ultimate 3000 system coupled with a TSQ Quantiva mass spectrometer was applied to determine the cellular concentration of compound FB23 and FB23-2. Analytes were separated on a XSELECT HSS T3 column (100 mm × 3.0 mm, 2.5 μm). The mobile phases used for elution were (A) 0.1% (v/v) formic acid/water and (B) 0.1% (v/v) formic acid/acetonitrile. The mass spectrometer was operated in the negative MRM mode. Parent-to-product transitions were m/z 375.1→339.1, 375.1→298.1 for FB23, and m/z 390.3→318.0, 390.3→289.9 for FB23-2, respectively.
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• Animal Research:
  The NSGS mice were bred and subjected to the xeno-transplantation model. For the AML mouse model, 0.2 × 10^6 MONOMAC6 cells were directly transplanted into NSGS mice via tail vein. After 10 days, FB23-2 (2 mg/kg/day) and DMSO vehicle were intraperitoneally injected into the mice for a continuous 10 days. The mice were euthanized by CO2 inhalation if they exhibited classical AML symptoms including hunched posture, paralysis, and reduced body weight. Meanwhile, the PB, spleen, and liver samples were collected for further analysis.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, leukemia, FB23 2, FB232, FB-23-2, FB23-2, m6A, myeloid, mRNA, mRNA N6-methyladenosine (m6A) demethylase FTO, inhibit, anti-proliferation, Apoptosis, AML, acute, demethylase

Compound Identifiers

PubChem CID

138454779