2. PROTAC Apoptosis Autophagy
  3. Ligands for E3 Ligase Autophagy Apoptosis
  4. Thalidomide

Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

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Thalidomide Chemical Structure

Thalidomide Chemical Structure

CAS No. : 50-35-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of Thalidomide:

Thalidomide Related Antibodies

Top Publications Citing Use of Products

    Thalidomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Thalidomide purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    H9 hESC are treated with increasing concentrations of Thalidomide, Lenalidomide, Pomalidomide, or DMSO as a control. Following 24 h of incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Thalidomide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 May 22;8:15398.  [Abstract]

    HEK293T cells are treated with 50 μg/mL Cycloheximide and increasing concentrations of Lenalidomide, Thalidomide or with DMSO, and cells are incubated for 6 h. ZFP91 and GAPDH levels are detected using anti-ZFP91 or anti-GAPDH immunoblotting.

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    von Hippel-Lindau (VHL) MDM2 Cereblon IAP

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.

    IC50 & Target

    Cereblon

     

    Cellular Effect
    Cell Line Type Value Description References
    DLD-1 IC50
    > 50 μM
    Compound: Thalidomide
    Cytotoxicity against human DLD1 cells by MTT assay
    Cytotoxicity against human DLD1 cells by MTT assay
    		[PMID: 19394719]
    Ehrlich IC50
    0.26 nM
    Compound: Thalidomide
    Cytotoxicity against mouse Ehrlich cells assessed as cell growth inhibition incubated for 3 hrs by trypan blue exclusion assay
    Cytotoxicity against mouse Ehrlich cells assessed as cell growth inhibition incubated for 3 hrs by trypan blue exclusion assay
    		[PMID: 34710743]
    HL-60 IC50
    > 50 μM
    Compound: Thalidomide
    Cytotoxicity against human HL60 cells by MTT assay
    Cytotoxicity against human HL60 cells by MTT assay
    		[PMID: 19394719]
    HT-29 IC50
    > 50 μM
    Compound: Thalidomide
    Cytotoxicity against human HT-29 cells by MTT assay
    Cytotoxicity against human HT-29 cells by MTT assay
    		[PMID: 19394719]
    HUVEC IC50
    > 50 μM
    Compound: Thalidomide
    Cytotoxicity against HUVEC by MTT assay
    Cytotoxicity against HUVEC by MTT assay
    		[PMID: 19394719]
    PBMC IC50
    ~ 200 μM
    Compound: Thalidomide
    Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC
    Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC
    		[PMID: 9873600]
    PBMC IC50
    77 μM
    Compound: 3
    Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA
    Inhibition of TNF-alpha production in LPS-stimulated human PBMC preincubated for 1 hr before LPS challenge measured after 28 to 20 hrs by ELISA
    		[PMID: 23168019]
    ST486 IC50
    > 50 μM
    Compound: Thalidomide
    Cytotoxicity against human ST486 cells by MTT assay
    Cytotoxicity against human ST486 cells by MTT assay
    		[PMID: 19394719]
    T-cell EC50
    > 10 μM
    Compound: 3
    Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA
    Inhibition of IL-2 production in human T cells measured after 2 to 3 days by ELISA
    		[PMID: 23168019]
    WI-38 IC50
    > 100 μg/mL
    Compound: 10 (Thalidomide)
    The cytotoxicity assessed using human embryonic lung fibroblast WI-38 cells.
    The cytotoxicity assessed using human embryonic lung fibroblast WI-38 cells.
    		[PMID: 9288167]
    In Vitro

    Thalidomide has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, and targets cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ～250 nM[1].
    Thalidomide (50 μg/mL) potentiates the anti-tumor activity of Icotinib against the proliferation of both PC9 and A549 cells, and this effect is correlated with apoptosis and cell migration. In addition, Thalidomide and Icotinib inhibits the EGFR and VEGF-R2 pathways in PC9 cells[3].

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

    Thalidomide Related Antibodies
    In Vivo

    Thalidomide (100 mg/kg, p.o.) inhibits the collagen deposition, down-regulates the mRNA expression level of α-SMA and collagen I, and significantly reduces the pro-inflammatory cytokines in RILF mice. Thalidomide alleviates RILF via suppression of ROS and down-regulation of TGF-β/Smad pathway dependent on Nrf2 status[2].
    Thalidomide (200 mg/kg, p.o.) combined with Icotinib shows synergistic anti-tumor effects in nude mice bearing PC9 cells, suppressing tumor growth and promoting tumor death[3].

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

    258.23

    Formula

    C13H10N2O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1N(C2CCC(NC2=O)=O)C(C3=CC=CC=C31)=O
    Shipping

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

    DMSO : 100 mg/mL (387.25 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 3.8725 mL 19.3626 mL 38.7252 mL
    5 mM 0.7745 mL 3.8725 mL 7.7450 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (9.68 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 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:  0.5% CMC-Na/saline water

      Solubility: 20 mg/mL (77.45 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% Tween-80 in PBS

      Solubility: 20 mg/mL (77.45 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 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

    Purity: 99.92%

    SDS (584 KB)

    COA (251 KB) HNMR (267 KB) RP-HPLC (243 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    THP-1 cells, A549 cells and KYSE30 cells are cultured in RPMI-1640 Medium supplemented with 10% fetal bovine serum and maintained at 37 °C in an atmosphere of 5% CO2 and 95% room air. THP-1 cells is irradiated with a single dose of 4 Gy 6-MV X-ray and treated with or without Thalidomide (0.2 μmol/mL)-containing medium for 48 h after radiation. The concentration of Thalidomide is selected based on the preliminary results[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    A total of 24 WT C57BL/6 mice are randomly divided into 4 groups for the experiments (n = 6 in each group): a control group, an irradiated group, a group irradiated along with Thalidomide, and a Thalidomide only group. Based on the preliminary results, 100 mg/kg Thalidomide is used in the experiment. Thalidomide is dissolved in DMSO vehicle. The treatment group receives the indicated dose of Thalidomide in 200  μL by gavage every other day beginning on day 1 for six treatments. The control mice receives 200 μL 0.1% DMSO contained-saline only. The lungs are harvested at 12 weeks after irradiation for the analysis. A total of 20 Nrf2-/- mice are randomly divided into 4 groups for the experiments (n = 5 in each group). The experiment procedures of Nrf2-/- mice are the same as WT C57BL/6 mice. In addition, a total of 30 WT C57BL/6 mice are randomly divided into 5 groups for the subsequent experiments (n = 6 in each group): a control group, an irradiated group, a group irradiated along with CDDO-Me and Thalidomide, a group irradiated along with CDDO-Me, and a group irradiated along with Thalidomide. 600 ng and 100 mg/kg are selected as the dose of CDDO-Me and Thalidomide for the experiment, respectively. The treatment group receives the indicated dose of CDDO-Me or Thalidomide in 200 μL by gavage every other day beginning on day 1 for six times. For the combined group of CDDO-Me and Thalidomide, CDDO-Me is delivered in 200 μL by gavage every other day beginning on day 1 for six treatments. Thalidomide is delivered in 200  μL by gavage every other day beginning on day 2 for six treatments[2].

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.8725 mL 19.3626 mL 38.7252 mL 96.8129 mL
    5 mM 0.7745 mL 3.8725 mL 7.7450 mL 19.3626 mL
    10 mM 0.3873 mL 1.9363 mL 3.8725 mL 9.6813 mL
    15 mM 0.2582 mL 1.2908 mL 2.5817 mL 6.4542 mL
    20 mM 0.1936 mL 0.9681 mL 1.9363 mL 4.8406 mL
    25 mM 0.1549 mL 0.7745 mL 1.5490 mL 3.8725 mL
    30 mM 0.1291 mL 0.6454 mL 1.2908 mL 3.2271 mL
    40 mM 0.0968 mL 0.4841 mL 0.9681 mL 2.4203 mL
    50 mM 0.0775 mL 0.3873 mL 0.7745 mL 1.9363 mL
    60 mM 0.0645 mL 0.3227 mL 0.6454 mL 1.6135 mL
    80 mM 0.0484 mL 0.2420 mL 0.4841 mL 1.2102 mL
    100 mM 0.0387 mL 0.1936 mL 0.3873 mL 0.9681 mL
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    Thalidomide 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:

    Thalidomide50-35-1Ligands for E3 LigaseAutophagyApoptosisE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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