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Catalog No.S1193

21 publications

Thalidomide Chemical Structure

CAS No. 50-35-1

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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Selleck's Thalidomide has been cited by 21 publications

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Choose Selective E3 ligase Ligand 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.
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 M13WTmZ2dmO2aX;uJIF{e2G7 M3LLSmlvcGmkaYTpc44hd2ZiSVytNU1idHCqYT3pcoR2[2WmIF7GMYtieHCjQjDhZ5RqfmG2aX;uJIlvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZoxw[2urbnegc4YheDVyL4C2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25uIFnDOVA:Oi5yNDFOwG0> NGXNS4IyPzh2NUi1NC=>
mouse RAW264.7 cells MoLTSpVv[3Srb36gZZN{[Xl? NYTmeWV3OTBizszN M4rDelMhcA>? M3HoSHJm\HWldHnvckBqdiCyRWLLNU8zKGW6cILld5Nqd25iaX6gUHBUNWGldHn2ZZRm\CCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDheEAyOCC3TTDwdoV1emWjdHXkJIZweiB|IHjyd{Bj\W[xcnWgUHBUKGOqYXzs[Y5o\SCjc4Pld5Nm\CCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2 NVu0TnVtOTh5MkOzOVc>
mouse RAW264.7 cells NV;I[ok{TnWwY4Tpc44h[XO|YYm= MoLPNVAh|ryP M33Td3Jm\HWldHnvckBqdiCrTl;TJIV5eHKnc4Ppc44hcW5iTGDTMYFkfGm4YYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjdDCxNEB2VSCycnX0doVifGWmIH\vdkA{KGi{czDi[YZwemViTGDTJINp[WyuZX7n[UBie3Onc4Pl[EBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91 Mni5NVg4OjN|NUe=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-p38 / p38 / Acetyl-H4 ; 

PubMed: 17620452     

Thalidomide induces activation of p38 MAPK and acetylation of histone H4. CD34+ cells were cultured in EPO alone medium for 7 days prior to the addition of thalidomide. (A) Cells were treated with different concentrations of thalidomide for 30 minutes. (B) Cells were treated with 100 μM thalidomide for the indicated times. Cellular protein (30 μg) was analyzed by Western blot using phosphorylated p38 MAPK and acetyl-histone H4 antibodies. The membranes were stripped and reprobed with total p38 MAPK and histone H4 antibodies as indicated to confirm that similar amounts of protein extracts were analyzed in each lane.


PubMed: 25053990     

Thalidomide regulates bFGF expression and cellular distribution in U266 cells. Immunofluorescence detection of bFGF in U266 cells treated with thalidomide for 4 h. Cellular distribution of bFGF was studied by fluorescence microscopy. DNA was stained with H33258 as a nuclear marker. Magnification, × 630.

VCAM-1/CUL5 / NEDD8 ; 

PubMed: 29746508     

CUL5 and NEDD8 colocalization in control cells treated with thalidomide (50 μg/mL) for 15 and 45 min, respectively. Immunostaining with anti- CUL5 and anti NEDD8 antibodies and nuclear DAPI staining was performed as described in the Methods. Images are of merged pictures from CUL5 staining (FITC-green) and NEDD8 staining (Texas red). Magnification is 40X.

25053990 29746508
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]


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.

* 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


CAS No. 50-35-1
Storage powder
in solvent
Synonyms N/A
Smiles C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04680195 Not yet recruiting Drug: Thalidomide Chronic Radiation Proctitis Sixth Affiliated Hospital Sun Yat-sen University December 14 2020 Phase 2
NCT02956538 Unknown status Drug: Thalidomide|Drug: placebo(for thalidomide) Crohn Disease Sixth Affiliated Hospital Sun Yat-sen University October 2016 Early Phase 1
NCT02966522 Unknown status Drug: Thalidomide|Drug: Dexamethasone Cardiac Amyloidosis Seoul National University Hospital|CW pharmaceutical company October 2016 Phase 2
NCT02778893 Unknown status Drug: Conmana|Drug: Thalidomide NSCLC Henan Provincial People''s Hospital March 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID