Homoharringtonine

SKU: orb1304259

Description

Homoharringtonine is a cytotoxic alkaloid that inhibits protein synthesis by blocking the elongation step of translation in ribosomes. It is widely used in cancer research, demonstrating antitumor activity in both in vitro cell studies and in vivo animal models for various malignancies.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 26833-87-4
• MW: 545.6
• Purity: >95%
• Formula: C₂₉H₃₉NO₉
• SMILES: COC(=O)CC(O)(CCCC(C)(C)O)C(=O)OC1C2c3cc4OCOc4cc3CCN3CCCC23C=C1OC
• Target: Ribosome
• Solubility: Soluble in DMSO (up to 75 mg/ml)

Bioactivity

• Target IC50:
  A549 cells growth:0.03 μM (SRB method)|K562 cells proliferation:0.014 μM (72h,CCK8 assay)|L02 cells growth:0.064 μM (72h,CCK8 assay)|A549 cells proliferation:31.6 nM (48h,MTT assay)|BaF3 cells proliferation:0.081 μM (72h,CCK8 assay)|HeLa cells proliferation:1.7 μM (68h, MTS assay)|A204 cells proliferation:0.004 μM (72h,CCK8 assay)|HeLa cells proliferation:0.4 μM (48h, MTT assay)|MDA-MB-453 cells growth:0.021 μM (72h,CCK8 assay)|4T1 cells proliferation:0.06 μM (72h,CCK8 assay)|HepG2 cells proliferation:34.5 nM (48h,MTT assay)|Huh7 cells proliferation:0.04 μM (72h,CCK8 assay)|KB cells growth:0.004 μM (SRB method)|HL-60 cells proliferation:0.013 μM (72h,CCK8 assay)|HCT116 cells proliferation:0.013 μM (72h,CCK8 assay)
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• In Vivo:
  METHODS: To detect anti-tumor activity in vivo, Homoharringtonine (10 mg/kg) was intraperitoneally injected five times a week for three weeks into nude immunodeficient mice harboring human lung cancer tumor H1975. RESULTS: Homoharringtonine effectively inhibited tumor growth, and STAT3 phosphorylation and MCL1 levels were significantly reduced in the Homoharringtonine-treated group. METHODS: To investigate the antitumor activity in vivo, Homoharringtonine (0.7 mg/kg) was administered by gavage to NOD/SCID mice bearing ccRCC tumor grafts twice daily for 28 days. RESULTS: Two tumor graft lines, XP26 and XP144, showed observable tumor growth inhibition following Homoharringtonine treatment. For XP26 tumors, tumor growth was inhibited by 63.7% in Homoharringtonine-treated mice compared to vector-treated mice, while tumor growth was inhibited by 43.0% in XP144 mice.
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• In Vitro:
  METHODS: Human lung cancer cells A549 and NCI-H1975 were treated with Homoharringtonine (1-6 µM) for 24-48 h. Cell viability was measured by MTT assay. RESULTS: Homoharringtonine was moderately cytotoxic to A549 with an IC50 of 3.7 µM. H1975 cells were more sensitive to Homoharringtonine with an IC50 of 0.7 µM. METHODS: Melanoma cells A375 and B16F10 were treated with Homoharringtonine (100 nM) for 48 h. Cell cycle and apoptosis were detected by Flow cytometry. RESULTS: Homoharringtonine induced apoptosis and G2/M cell cycle arrest in A375 and B16F10 cells.
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• Cell Research:
  Homoharringtonine (HHT) is dissolved in PBS at a stock solution of 2.5 mM and kept at 20°C. Human NSCLC cell lines MCF-10A, A549 and H1975 cells are seeded into 96-well plate and precultured for 24 h, then treated with Homoharringtonine for 24 h or 48 h. Cell cytotoxicity is determined by MTT assay. The absorbance is measured at 570 nm by Varioskan Flash Multimode Reader, and the cell death rate is calculated. Cell viability is estimated by trypan blue dye exclusion assay. The cells which exclude the dye are viable. Place 0.5 mL of a suitable cell suspension (dilute cells in complete medium without serum to 1×106 cells per mL) following adding 0.1 mL of 0.4% trypan blue dye and mixing thoroughly, and then incubate at room temperature for 3 min and load into a hemacytometer to count cells in three separate fields (nonviable, deep blue cells as well as viable, clear cells). The cell viability rate is calculated. After staining with Hoechst 33258 at 10 mg/mL for 10 min, cell death is observed by a fluorescence microscope.
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Storage & Handling

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

Alternative Names

HHT; NSC 141633; Omacetaxine mepesuccinate

Compound Identifiers

PubChem CID

3628