APTO-253

SKU: orb1309990

Description

APTO-253 is a small molecule that stabilizes G-quadruplex DNA, leading to c-Myc downregulation and KLF4 tumor suppressor induction. This mechanism results in cell cycle arrest and apoptosis in acute myeloid leukemia (AML) cells, as demonstrated in in vitro studies. Its activity makes it a candidate for oncology research, particularly in hematological malignancies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 916151-99-0
• MW: 367.38
• Purity: 99.43% (May vary between batches)
• Formula: C₂₂H₁₄FN₅
• SMILES: Cc1[nH]c2ccc(F)cc2c1-c1nc2c([nH]1)c1cccnc1c1ncccc21
• Target: Apoptosis,KLF,c-Myc
• Solubility: DMSO:35.71 mg/mL (97.2 mM)

Bioactivity

• In Vitro:
  APTO-253 (5 μM) induces KLF4 expression and enhances apoptosis induced by NSC 119875 in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells . APTO-253 is cytotoxic to Raji and Raji/253R cell lines (IC50s: 105 nM and 1387 nM). APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R . APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines (IC50s: 57 nM to 1.75 μM). APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down-regulates MYC RNA and protein expression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells. Furthermore, APTO-253 is a potent stabilizer of G-quadruplex (G4) motifs and demonstrates the greatest propensity for stabilizing the MYC G4 sequences.

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

cMyc, c-Myc, Apoptosis, APTO253, APTO-253, APTO 253, LT253, LT-253, LT 253, inhibit, Myc, KLF, Krüppel-like factor, LOR 253, LOR253, LOR-253, Inhibitor

Compound Identifiers

PubChem CID

11960271