الصفحة الرئيسية>>Signaling Pathways>> JAK/STAT Signaling>> STAT>>Homoharringtonine

Homoharringtonine (Synonyms: NSC 141633, Omacetaxine Mepesuccinate)

رقم الكتالوجGN10742

Homoharringtonine is a protein synthesis inhibitor and a cytotoxic alkaloid, originally isolated from the evergreen tree Cephalotaxus hainanensis. It is often used in the research of lung cancer and breast cancer.

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Homoharringtonine التركيب الكيميائي

Cas No.: 26833-87-4

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
59٫00
متوفر
5mg
49٫00
متوفر
10mg
61٫00
متوفر
50mg
168٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of Homoharringtonine

Homoharringtonine is a protein synthesis inhibitor and a cytotoxic alkaloid, originally isolated from the evergreen tree Cephalotaxus hainanensis. It is often used in the research of lung cancer and breast cancer[1].

Homoharringtonine (0-36.7nM; 0-96h) effectively inhibits the growth and viability of human acute myeloid leukemia cells and promotes cell cycle arrest, apoptosis and differentiation[1]. Homoharringtonine (0-400nM; 24-48h) inhibits the proliferation of melanoma cells A375 and B16F10 in vitro by inducing DNA damage, apoptosis, and G2/M cell cycle arrest[2]. Homoharringtonine (20nM; 0-48h) suppresses tumor proliferation and migration by regulating EphB4-mediated β-catenin loss in hepatocellular carcinoma[3].

In an A375 cell xenograft mice model, Homoharringtonine (1mg/kg; 10 days) can treat mice FLT3 mutant acute myeloid leukemia by targeting the SP1/TET1 pathway in acute myeloid leukemia cells and downregulating overall 5hmC levels[1]. Homoharringtonine (2.5mg/kg; two-day intervals; 20 days) inhibits the growth of lung tumor cells in mice carrying Kras mutations in vivo by altering cytokine expression in immune cells through inhibition of protein synthesis[4].

References:
[1]. Li C, Dong L, Su R, et al. Homoharringtonine exhibits potent anti-tumor effect and modulates DNA epigenome in acute myeloid leukemia by targeting SP1/TET1/5hmC[J]. haematologica, 2020, 105(1): 148.
[2]. Tang J, Li G, Zhang T, et al. Homoharringtonine inhibits melanoma cells proliferation in vitro and vivo by inducing DNA damage, apoptosis, and G2/M cell cycle arrest[J]. Archives of Biochemistry and Biophysics, 2021, 700: 108774.
[3]. Zhu, Man et al. “Homoharringtonine suppresses tumor proliferation and migration by regulating EphB4-mediated β-catenin loss in hepatocellular carcinoma.” Cell death & disease vol. 11,8 632. 14 Aug. 2020.
[4]. Weng T Y, Wu H F, Li C Y, et al. Homoharringtonine induced immune alteration for an efficient anti-tumor response in mouse models of non-small cell lung adenocarcinoma expressing Kras mutation[J]. Scientific reports, 2018, 8(1): 8216.

Protocol of Homoharringtonine

Cell experiment [1]:

Cell lines

A375 and B16F10 cells

Preparation Method

The A375 and B16F10 cells were treated with different concentrations of Homoharringtonine (0-400nM) for 24 and 48h.

Reaction Conditions

0-400nM; 24-48h

Applications

The colony formation, proliferation, and the cell cycle of A375 and B16F10 cells were inhibited obviously after treating with Homoharringtonine.
Animal experiment [2]:

Animal models

KrasG12D-expressing LL2 tumor modle

Preparation Method

KrasG12D-expressing LL2 cells (2×105 cells in 200μl of PBS) were injected via the subcutaneous (s.c.) route into C57/BL6 mice. Tumor-bearing mice received intraperitoneal (i.p.) injections of Homoharringtonine (1.25-2.5 mg/kg) on day 10 after the tumor challenge, at two-day intervals, with a total of 10 i.p. injections administered.

Dosage form

1.25-2.5mg/kg; ip; two-day intervals, 20 days

Applications

Homoharringtonine inhibited the growth of mouse lung tumor cells carrying Kras mutation in vivo, and decreased expression of endogenous ERK, STAT3, and Akt was observed in lung tumor cells.

References:
[1]. Tang J, Li G, Zhang T, et al. Homoharringtonine inhibits melanoma cells proliferation in vitro and vivo by inducing DNA damage, apoptosis, and G2/M cell cycle arrest[J]. Archives of Biochemistry and Biophysics, 2021, 700: 108774.
[2]. Weng T Y, Wu H F, Li C Y, et al. Homoharringtonine induced immune alteration for an efficient anti-tumor response in mouse models of non-small cell lung adenocarcinoma expressing Kras mutation[J]. Scientific reports, 2018, 8(1): 8216

Chemical Properties of Homoharringtonine

Cas No. 26833-87-4 SDF
المرادفات NSC 141633, Omacetaxine Mepesuccinate
Chemical Name (R)-1-((11bS,12S,14aR)-13-methoxy-2,3,5,6,11b,12-hexahydro-1H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d]cyclopenta[b]pyrrolo[1,2-a]azepin-12-yl) 4-methyl 2-hydroxy-2-(4-hydroxy-4-methylpentyl)succinate
Formula C29H39NO9 M.Wt 545.62
الذوبان ≥ 181.2mg/mL in DMSO Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Homoharringtonine

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.8328 mL 9.1639 mL 18.3278 mL
5 mM 0.3666 mL 1.8328 mL 3.6656 mL
10 mM 0.1833 mL 0.9164 mL 1.8328 mL
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