Thalidomide

Catalog No.S1193

Thalidomide Chemical Structure

Molecular Weight(MW): 258.23

Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.

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Cited by 9 Publications

4 Customer Reviews

  • (E) MM.1S cells were treated with Thal(Thalidomide) or Pom for 48 hours. In each case, western blot was carried out using cell lysates and the indicated Abs.

    Blood, 2017, 129(10):1308-1319. Thalidomide purchased from Selleck.

    Thalidomide and lenalidomide increase the protein level of WT CRBN. Plasmids expressing FS-CRBN WT were transfected into HEK293T cells and then cells were equally divided into each well of a 6-well plate. The cells were treated with thalidomide (100 µM) or lenalidomide (10 µM) for indicated time.

    FASEB Journal, 2015, fj.15-274050. Thalidomide purchased from Selleck.

  • PC cells were treated with 100 μM thalidomide for 24 h, and EMT markers were detected (n=3/group)

    Oncotarget, 2016, 7(25):38539-38550. Thalidomide purchased from Selleck.

    Murine bone marrow-derived DC (cultured for 4 d) conferred thalidomide (30 μM), PYR-41 (5 μM), or DMSO treatment prior to ovalbumin (50 μg/ml) or PBS pulse. The effects of PYR-41 and thalidomide on cross-presentation were determined by confocal microscope (b). For immunofluorescence observations, cross-presented OVA was stained with red (25-D1.16), EEA1 and Rab7 are all stained with green, and nuclei were counterstained with blue (DAPI). Original magnification, ×600.

    J Immunol Res, 2018, 2018:5070573. Thalidomide purchased from Selleck.

Purity & Quality Control

Choose Selective E3 Ligase Inhibitors

Biological Activity

Description Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits an E3 ubiquitin ligase, which is a CRBN-DDB1-Cul4A complex.
Targets
E3 Ligase [6]
(Cell-free assay)
TNF-alpha [2]
(Cell-free assay)
In vitro

Thalidomide must be metabolized by the liver to form an epoxide that may be the active teratogenic metabolite. [1] Thalidomide selectively inhibits the production of human monocyte tumor necrosis factor alpha (TNF-alpha) when human monocytes are triggered with lipopolysaccharide and other agonists in culture. [2] Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. [3] Thalidomide acts directly, by inducing apoptosis or G1 growth arrest, in MM cell lines and in patient MM cells that are resistant to melphalan, doxorubicin, and dexamethasone (Dex). Thalidomide enhances the anti-MM activity of Dex and, conversely, are inhibited by interleukin 6. [4] Thalidomide is a potent costimulator of primary human T cells in vitro, synergizing with stimulation via the T cell receptor complex to increase interleukin 2-mediated T cell proliferation and interferon gamma production. Thalidomide also increases the primary CD8+ cytotoxic T cell response induced by allogeneic dendritic cells in the absence of CD4+ T cells. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells MkL4SpVv[3Srb36gZZN{[Xl? M17CcGlvcGmkaYTpc44hd2ZiSVytNU1idHCqYT3pcoR2[2WmIF7GMYtieHCjQjDhZ5RqfmG2aX;uJIlvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZoxw[2urbnegc4YheDVyL4C2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25uIFnDOVA:Oi5yNDFOwG0> NVu2V4VGOTd6NEW4OVA>
mouse RAW264.7 cells NEnuc2pHfW6ldHnvckBie3OjeR?= Mn[zNVAh|ryP M3vaSVMhcA>? MWXS[YR2[3Srb36gbY4heEWUS{GvNkBmgHC{ZYPzbY9vKGmwIFzQV{1i[3SrdnH0[YQhdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYSgNVAhfU1icILleJJm[XSnZDDmc5IhOyCqcoOgZoVnd3KnIFzQV{BkcGGubHXu[4Uh[XO|ZYPz[YQh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfA>? NUHwNGZ5OTh5MkOzOVc>
mouse RAW264.7 cells M3rtZmZ2dmO2aX;uJIF{e2G7 MWqxNEDPxE1? MVXS[YR2[3Srb36gbY4hcU6RUzDlfJBz\XO|aX;uJIlvKEySUz3hZ5RqfmG2ZXSgcY92e2ViUlHXNlY1NjdiY3XscJMh[XRiMUCgeW0heHKndILlZZRm\CCob4KgN{BpenNiYnXmc5JmKEySUzDjbIFtdGWwZ3WgZZN{\XO|ZXSgZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveC=> NYnLS3dLOTh5MkOzOVc>

... Click to View More Cell Line Experimental Data

In vivo Thalidomide (200 mg/kg) results in an inhibition of the area of vascularized cornea of rabbits that ranged from 30% to 51% in three experiments with a median inhibition of 36%. [1]

Protocol

Solubility (25°C)

In vitro DMSO 51 mg/mL (197.49 mM)
Ethanol 2 mg/mL (7.74 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+1% Tween 80+ddH2O (suspension)
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 258.23
Formula

C13H10N2O4

CAS No. 50-35-1
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03608501 Not yet recruiting Multiple Myeloma Takeda May 30 2019 Phase 2
NCT03608501 Not yet recruiting Multiple Myeloma Takeda May 30 2019 Phase 2
NCT03777930 Not yet recruiting Cancer Therapy-Related Shenzhen Fifth People''s Hospital December 10 2018 Phase 4
NCT03777930 Not yet recruiting Cancer Therapy-Related Shenzhen Fifth People''s Hospital December 10 2018 Phase 4
NCT03601871 Recruiting Chemotherapy-induced Nausea and Vomiting Yunpeng Liu|China Medical University China July 12 2018 Not Applicable
NCT03601871 Recruiting Chemotherapy-induced Nausea and Vomiting Yunpeng Liu|China Medical University China July 12 2018 Not Applicable

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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E3 Ligase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID