2. Autophagy
  3. Autophagy
  4. TFEB activator 1

TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.

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CAS No. : 39777-61-2

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Based on 10 publication(s) in Google Scholar

TFEB activator 1 Related Antibodies

Top Publications Citing Use of Products

    TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240.  [Abstract]

    TFEB activator 1 (TA1) (10 mg/kg; p.o.; once daily for 3 months) reduced Aβ plaques in the mouse brain.

    TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240.  [Abstract]

    TFEB activator 1 (TA1) (10 mg/kg; p.o.; once daily for 3 months) reduced Aβ load in the mouse cortex.

    TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240.  [Abstract]

    TFEB activator 1 (TA1) (10 mg/kg; p.o.; once daily for 3 months) upregulated the colocalization of Aβ with LC3 as well as the colocalization of LC3 with LAMP1 in PAM.

    TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240.  [Abstract]

    TFEB activator 1 (TA1) (1 μM; 12 h) upregulated the transcription activity of TFEB target genes Lamp1, Vps11, Wipi2, and Vps18 in PAM in vitro.

    TFEB activator 1 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2023 Oct 20;20(1):240.  [Abstract]

    PAMs were fixed and stained with anti-TFEB antibody and DAPI. Nuclear translocation of TFEB was measured by quantifying the intensity of TFEB in DAPI. TFEB activator 1 (TA1) (1 μM; 12 h) upregulated the nuclear levels of TFEB in PAM.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment[1].

    IC50 & Target

    EC50: 2167 nM (Flag-TFEB nuclear translocation)[1]
    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 GI50
    4 μM
    Compound: GO-Y019
    Growth inhibition of human HCT116 cells after 48 hrs by MTS assay
    Growth inhibition of human HCT116 cells after 48 hrs by MTS assay
    		[PMID: 20060305]
    HL-60 IC50
    < 12.6 μM
    Compound: B6
    Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
    Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
    		[PMID: 19243951]
    HeLa IC50
    161 μM
    Compound: B6
    Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
    Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
    		[PMID: 19243951]
    KB IC50
    < 12.6 μM
    Compound: B6
    Cytotoxicity against human KB cells after 72 hrs by MTT assay
    Cytotoxicity against human KB cells after 72 hrs by MTT assay
    		[PMID: 19243951]
    MDA-MB-231 GI50
    1 μM
    Compound: 29; GO-Y019
    Growth inhibition of human MDA-MB-231 cells measured after 72 hrs by microplate reader analysis
    Growth inhibition of human MDA-MB-231 cells measured after 72 hrs by microplate reader analysis
    		[PMID: 32172081]
    RPMI-7951 GI50
    2.3 μM
    Compound: 29; GO-Y019
    Growth inhibition of human RPMI-7951 cells measured after 72 hrs by microplate reader analysis
    Growth inhibition of human RPMI-7951 cells measured after 72 hrs by microplate reader analysis
    		[PMID: 32172081]
    In Vitro

    TFEB activator 1 (Compound C1) activates TFEB (transcription factor EB) by directly binding to TFEB and promotes its entry into the nucleus, without affecting TFEB phosphorylation or inhibiting the activities of MTOR and MAPK1/ERK2-MAPK3/ERK1[1].
    ? TFEB activator 1 (1 μM; for 12 h) significantly increases the levels of LC3B-II, the lipidated and phagophore- or autophagosome-associated form of MAP1LC3B/LC3B (microtubule-associated protein 1 light chain 3 β) in N2a cells[1].
    ? TFEB activator 1 (0.2-1 μM) dose-dependently increases the levels of LC3-II and SQSTM1/p62 (sequestosome 1) in N2a cells[1].

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

    TFEB activator 1 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: N2a cells
    Concentration: 0, 0.2, 0.4, 0.6, 0.8 and 1 μM
    Incubation Time: 12 hours
    Result: Treatment dose-dependently increased the levels of LC3-II and SQSTM1/p62 (sequestosome 1).
    In Vivo

    The medium lethal dose (LD50) value of TFEB activator 1 (Compound C1) is 175 mg/kg in the acute toxicity assay (single-dose i.v. tail vein injection; in rats) [1].
    ? Short-term oral administration of TFEB activator 1 (low dosage 10 mg/kg and high dosage 25 mg/kg; for 24 h) dose-dependently increases the expression of LC3B-II and TFEB in the liver, frontal cortex and striatum of the brain[1].
    ? Chronic administration of TFEB activator 1 (10 mg/kg per day; orally administered by gavage) activates TFEB and enhances autophagy in rat brains[1].

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

    Animal Model: Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g[1]
    Dosage: 10 mg/kg and 25 mg/kg
    Administration: Short-term oral administration; for 24 hours
    Result: Activated TFEB and enhanced autophagy and lysosome biogenesis in rat brain.
    Animal Model: Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g[1]
    Dosage: 10 mg/kg
    Administration: Chronic oral administration; daily; for 21 days
    Result: Activated TFEB and enhanced autophagy in rat brains.
    Molecular Weight

    294.34

    Formula

    C19H18O3
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(/C=C/C1=CC=CC=C1OC)/C=C/C2=CC=CC=C2OC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (424.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3974 mL 16.9872 mL 33.9743 mL
    5 mM 0.6795 mL 3.3974 mL 6.7949 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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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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    C2

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    90% Corn Oil

      Solubility: ≥ 6.25 mg/mL (21.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  50% PEG300    50% Saline

      Solubility: 4 mg/mL (13.59 mM); Suspended solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *The compound is unstable in solutions, freshly prepared is recommended.

    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3974 mL 16.9872 mL 33.9743 mL 84.9358 mL
    5 mM 0.6795 mL 3.3974 mL 6.7949 mL 16.9872 mL
    10 mM 0.3397 mL 1.6987 mL 3.3974 mL 8.4936 mL
    15 mM 0.2265 mL 1.1325 mL 2.2650 mL 5.6624 mL
    20 mM 0.1699 mL 0.8494 mL 1.6987 mL 4.2468 mL
    25 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3974 mL
    30 mM 0.1132 mL 0.5662 mL 1.1325 mL 2.8312 mL
    40 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1234 mL
    50 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
    60 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4156 mL
    80 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
    100 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8494 mL
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    TFEB activator 1 Related Classifications

    Help & FAQs
    • 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:

    TFEB activator 139777-61-2TFEB activator1TFEB activator-1AutophagyorallyeffectivemTOR-independentTFEBneurodegenerativediseaseInhibitorinhibitorinhibit

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