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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3 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.

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 NI\LPWxHfW6ldHnvckBie3OjeR?= MVfJcohq[mm2aX;uJI9nKEmOLUGtZYxxcGFvaX7keYNm\CCQRj3rZZBx[UJiYXP0bZZifGmxbjDpckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IHLsc4NscW6pIH;mJJA2OC:yNkWgcpVkdGWjcjD0doFve2yxY3H0bY9vNCCLQ{WwQVIvODRizszN NUD3UJo3OTd6NEW4OVA>
mouse RAW264.7 cells M1PqXmZ2dmO2aX;uJIF{e2G7 M1PR[|ExKM7:TR?= NHHHW2E{KGh? MYDS[YR2[3Srb36gbY4heEWUS{GvNkBmgHC{ZYPzbY9vKGmwIFzQV{1i[3SrdnH0[YQhdW:3c3WgVmFYOjZ2LkegZ4VtdHNiYYSgNVAhfU1icILleJJm[XSnZDDmc5IhOyCqcoOgZoVnd3KnIFzQV{BkcGGubHXu[4Uh[XO|ZYPz[YQh[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfA>? M1G5RlE5PzJ|M{W3
mouse RAW264.7 cells MojlSpVv[3Srb36gZZN{[Xl? NXXIUI9WOTBizszN NVrqV4F7WmWmdXP0bY9vKGmwIHnOU3Mh\XiycnXzd4lwdiCrbjDMVHMu[WO2aY\heIVlKG2xdYPlJHJCXzJ4ND63JINmdGy|IHH0JFExKHWPIIDy[ZRz\WG2ZXSg[o9zKDNiaILzJIJm\m:{ZTDMVHMh[2ijbHzlcodmKGG|c3Xzd4VlKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3R? MW[xPFczOzN3Nx?=

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
5 mg/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
NCT03016000 Not yet recruiting Lymphoma, Large B-Cell, Diffuse Nanfang Hospital of Southern Medical University February 2017 Phase 3
NCT02891811 Not yet recruiting Multiple Myeloma Arbeitsgemeinschaft medikamentoese Tumortherapie|Amgen January 2017 Phase 2
NCT03004287 Not yet recruiting Multiple Myeloma University of Arkansas|Janssen, LP January 2017 Phase 2
NCT02998827 Enrolling by invitation Crohn Disease Sixth Affiliated Hospital, Sun Yat-sen University November 2016 --
NCT02966522 Recruiting Cardiac Amyloidosis Seoul National University Hospital|CW pharmaceutical company October 2016 Phase 2
NCT02956538 Recruiting Crohn Disease Sixth Affiliated Hospital, Sun Yat-sen University October 2016 Early Phase 1

Tech Support

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E3 Ligase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID