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  4. Colchicine

Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs).

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Colchicine Chemical Structure

Colchicine Chemical Structure

CAS No. : 64-86-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 32 publication(s) in Google Scholar

Other Forms of Colchicine:

Top Publications Citing Use of Products

    Colchicine purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2020 Jul 15;2020:9173530.  [Abstract]

    Colchicine plays an antipyroptosis role by inhibiting intracellular oxidative stress. HUVECs are treated for 10 or 24 h with different doses of Colchicine (0-10 nM) in the presence of cholesterol crystal (0.5 mg/mL). Intracellular ROS level is detected using a DCFH-DA probe. JC-1 Staining Kit is used for the detection of mitochondrial membrane potential.

    Colchicine purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2020 Jul 15;2020:9173530.  [Abstract]

    Colchicine alleviates NLRP3 inflammasome activation relevant in pyroptosis. HUVECs are treated for 24 h with different doses of Colchicine (0-10 nM) in the presence of cholesterol crystal (0.5 mg/mL. Western blotting Is dedicated to examine the protein expression levels of NLRP3, ASC-1, procaspase-1, caspase-1, IL-18, and IL-1β. Colchicine treatment significantly blocks NLRP3 signal activity. Colchicine significantly inhibits CC-induced mRNA and protein expression of IL-18 and IL-1β, particularl

    Colchicine purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2018 May;1862(5):1134-1147.  [Abstract]

    CS1 and Colchicine (Col) induce the phosphorylation of H1 (T18) and H3 (S29) as detected by western blotting.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM[1][2][3]. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs)[4].

    IC50 & Target

    Microtubule/Tubulin[1]

    In Vitro

    Exposure to 1μM Colchicine, a microtubule disrupting agent, triggered apoptosis in rat cerebellar granule cells (CGC). Colchicine treatment also causes alterations in Ca2+ responses to chemical depolarization and a moderate, but progressive, increase in the resting intracellular Ca2+ concentration[1]. Colchicine exerts its biological effects through binding to the soluble tubulin heterodimer, the major component of the microtubule. The Colchicine binding abilities of tubulins from a variety of sources are summarized, and the mechanism of Colchicine binding to brain tubulin is explored in depth. The relationship between colchicinoid structure and tubulin binding activity provides insight into the structural features of Colchicine responsible for high affinity binding to tubulin and is reviewed for analogs in the Colchicine series. The thermodynamic and kinetic aspects of the association are described and evaluated in terms of the binding mechanism. Colchicine binding to tubulin results in unusual alterations in the low energy electronic spectra of Colchicine. The spectroscopic features of Colchicine bound to tubulin are discussed in terms of the nature of the Colchicine-tubulin complex. Attempts to locate the high affinity Colchicine binding site on tubulin are presented[2]. Colchicine treatment inhibits indomethacin-induced small intestinal injury by 86% (1 mg/kg) and 94% (3 mg/kg) as indicated by the lesion index 24 h after indomethacin administration. Colchicine inhibits the protein expression of cleaved caspase-1 and mature IL-1β, without affecting the mRNA expression of NLRP3 and IL-1β[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Vehicle or Colchicine (1 mg/kg) is administered orally 30 min prior to indomethacin administration. The lesions stained with Evans blue in the small intestine are smaller in Colchicine-treated mice than those in vehicle-treated mice 24 h after indomethacin administration. In addition, histological examination shows that Colchicine-treated mice have less mucosal inflammation and ulceration and a decrease in the size and numbers of lesions compared with vehicle-treated mice. Colchicine treatment significantly reduces the lesion index at doses of 1 mg/kg and 3 mg/kg (by 86% and 94%, respectively) compared with vehicle treatment. Colchicine treatment significantly inhibits the protein levels of mature IL-1β at doses of 1 mg/kg and 3 mg/kg (by 56% and 69%, respectively) without affecting those of pro-IL-1β. Colchicine treatment also significantly inhibits the protein levels of cleaved caspase-1 at doses of 1 mg/kg and 3 mg/kg (by 26% and 39%, respectively) without affecting those of pro-caspase-1[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    399.44

    Formula

    C22H25NO6

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CC(N[C@H](C1=C2)CCC3=CC(OC)=C(OC)C(OC)=C3C1=CC=C(OC)C2=O)=O

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 48 mg/mL (120.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : ≥ 33.33 mg/mL (83.44 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5035 mL 12.5175 mL 25.0350 mL
    5 mM 0.5007 mL 2.5035 mL 5.0070 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 2.78 mg/mL (6.96 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.91%

    References
    Animal Administration
    [3]

    Mice[3]
    Specific-pathogen-free 8-week-old male mice are used. Wild-type C57BL/6 mice and NLRP3−/− mice on a C57BL/6 background are used. To examine the effects of Colchicine on NSAID-induced small intestinal injury, vehicle or Colchicine (1 or 3 mg/kg) is administered orally 30 min prior to indomethacin administration. Mice received intraperitoneal injections of sterilized phosphate buffered saline or mouse recombinant IL-1β (0.1 μg/kg) 3 h after indomethacin treatment. Vehicle or Colchicine (1 or 3 mg/kg) is also administered to NLRP3−/− mice before indomethacin administration. The lesion index is evaluated 24 h after indomethacin administration, and examined mRNA and protein expression of inflammasome components 6 h after indomethacin administration.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.5035 mL 12.5175 mL 25.0350 mL 62.5876 mL
    5 mM 0.5007 mL 2.5035 mL 5.0070 mL 12.5175 mL
    10 mM 0.2504 mL 1.2518 mL 2.5035 mL 6.2588 mL
    15 mM 0.1669 mL 0.8345 mL 1.6690 mL 4.1725 mL
    20 mM 0.1252 mL 0.6259 mL 1.2518 mL 3.1294 mL
    25 mM 0.1001 mL 0.5007 mL 1.0014 mL 2.5035 mL
    30 mM 0.0835 mL 0.4173 mL 0.8345 mL 2.0863 mL
    40 mM 0.0626 mL 0.3129 mL 0.6259 mL 1.5647 mL
    50 mM 0.0501 mL 0.2504 mL 0.5007 mL 1.2518 mL
    60 mM 0.0417 mL 0.2086 mL 0.4173 mL 1.0431 mL
    80 mM 0.0313 mL 0.1565 mL 0.3129 mL 0.7823 mL
    DMSO 100 mM 0.0250 mL 0.1252 mL 0.2504 mL 0.6259 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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