2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Cycloleucine

Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects.

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CAS No. : 52-52-8

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Based on 10 publication(s) in Google Scholar

Cycloleucine Related Antibodies

Top Publications Citing Use of Products

    Cycloleucine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Dec 25.

    The ratio of GAC/KGA in human HCC cell lines was detected using RT-qPCR after treatment with Cycloleucine (40 μM; 24 h).

    Cycloleucine purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Dec 25.

    Cycloleucine (40 μM; 24 h) treatment promoted KGA expression and reduced GAC expression in human HCC cell lines as measured by Western blotting analysis.

    Cycloleucine purchased from MedChemExpress. Usage Cited in: Neuron. 2025 Nov 4:S0896-6273(25)00755-X.  [Abstract]

    Cycloleucine (cLEU) (4 μg/μL; 120 nL per side; i.c.) significantly alleviated abdominal pain, hunching behaviors, and depression-like behaviors in PDAC mice.

    Cycloleucine purchased from MedChemExpress. Usage Cited in: Int J Oral Sci.2024 May 23;16(1):42.  [Abstract]

    Treated with Cycloleucine (500 µg/mL), representative images and quantitative analyses of ALP and ARS staining of BMSCs from Vector/oe-CORIN Group.

    Cycloleucine purchased from MedChemExpress. Usage Cited in: Int J Oral Sci.2024 May 23;16(1):42.  [Abstract]

    Cycloleucine (500 µg/mL) markedly decreased Runx2/OCN expression in BMSCs from the Vector/oe-CORIN group.

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    Description

    Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects[1][2][3][4].

    IC50 & Target

    NMDA Receptor

     

    In Vitro

    Cycloleucine (4-40 mM; 3 h) blocks internal methylation of viral RNA in B77 transformed chick embryo fibroblasts[5].
    Cycloleucine (40 mM; 24 h) blocks the formation of both m6A and the penultimate Gm in B77 38S RNA subunits by greater than 90%[5].
    Cytostatic (10 μg/mL) inhibits the viability human KB and mouse L1210s leukemia cell lines[5].

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

    Cycloleucine Related Antibodies
    In Vivo

    Cycloleucine (0.5-4 μg; intracerebroventrical injection) increases time spent in open arms, open arm entries, and extreme arrivals in rats[3]. Cycloleucine reduces thymus and spleen weights in Semliki Forest virus (SFV) strain A7(74) infected and control mice[6].

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

    Animal Model: Male rats bilaterally cannulated into the nucleus accumbens septi (NAS)[3]
    Dosage: 1 µL of 0.5, 1.0, 2.0, 4 µg/µL
    Administration: Intracerebroventrical injection
    Result: Increased time spent in the open arms and extreme arrivals at all doses.
    Increased open arm entries at the dose of 4 μg.
    Molecular Weight

    129.16

    Formula

    C6H11NO2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C1(CCCC1)N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 20 mg/mL (154.85 mM; Need ultrasonic)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 7.7423 mL 38.7117 mL 77.4233 mL
    5 mM 1.5485 mL 7.7423 mL 15.4847 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * 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)

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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: 100 mg/mL (774.23 mM); Clear solution; Need ultrasonic

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

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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: 98.0%

    SDS (479 KB)

    COA (251 KB) HNMR (237 KB)

    Handling Instructions (2659 KB)
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 7.7423 mL 38.7117 mL 77.4233 mL 193.5584 mL
    5 mM 1.5485 mL 7.7423 mL 15.4847 mL 38.7117 mL
    10 mM 0.7742 mL 3.8712 mL 7.7423 mL 19.3558 mL
    15 mM 0.5162 mL 2.5808 mL 5.1616 mL 12.9039 mL
    20 mM 0.3871 mL 1.9356 mL 3.8712 mL 9.6779 mL
    25 mM 0.3097 mL 1.5485 mL 3.0969 mL 7.7423 mL
    30 mM 0.2581 mL 1.2904 mL 2.5808 mL 6.4519 mL
    40 mM 0.1936 mL 0.9678 mL 1.9356 mL 4.8390 mL
    50 mM 0.1548 mL 0.7742 mL 1.5485 mL 3.8712 mL
    60 mM 0.1290 mL 0.6452 mL 1.2904 mL 3.2260 mL
    80 mM 0.0968 mL 0.4839 mL 0.9678 mL 2.4195 mL
    100 mM 0.0774 mL 0.3871 mL 0.7742 mL 1.9356 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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    Cycloleucine Related Classifications

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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.

    Keywords:

    Cycloleucine52-52-8iGluRIonotropic glutamate receptorsnucleicmethylationsATPtransferaseNMDAglycineanxiolyticcytostaticInhibitorinhibitorinhibit

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