Home Ubiquitin E3 ligase Ligand chemical - E3 Ligase inhibitor - TNF-alpha inhibitor Thalidomide For research use only.

Thalidomide

Synonyms: K17

Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.

Thalidomide Chemical Structure

Thalidomide Chemical Structure

CAS No. 50-35-1

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa Function assay Inhibition of IL-1-alpha-induced NF-kappaB activation in HeLa cells assessed as blocking of p50/p65 nuclear translocation, IC50=2.04μM 17845850
RAW264.7 Antiinflammatory assay 10 uM 3 hrs Antiinflammatory activity in mouse LPS-activated RAW264.7 cells assessed as ROS scavenging activity at 10 uM pretreated for 3 hrs before LPS challenge measured by decrease in fluorescent intensity by confocal microscopy 18723357
RAW264.7 Function assay 1 uM 3 hrs Reduction in iNOS expression in LPS-activated mouse RAW264.7 cells at 1 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot 18723357
RAW264.7 Function assay 10 uM 3 hrs Reduction in iNOS expression in LPS-activated mouse RAW264.7 cells at 10 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot 18723357
RAW264.7 Function assay 10 uM 3 hrs Reduction in pERK1/2 expression in LPS-activated mouse RAW264.7 cells at 10 uM pretreated for 3 hrs before LPS challenge assessed after 24 hrs by Western blot 18723357
Ehrlich ascites carcinoma cells Toxicity assay 1.25 mM/kg 7 days Toxicity in Swiss albino mouse bearing mouse Ehrlich ascites carcinoma cells assessed as focal degeneration of hepatocytes treated after 7 days post-tumor implantation at 1.25 mM/kg, sc for 5 days by histopathological analysis 18951804
Ehrlich ascites carcinoma cells Toxicity assay 1.25 mM/kg 7 days Toxicity in Swiss albino mouse bearing mouse Ehrlich ascites carcinoma cells assessed as focal necrosis of hepatocytes treated after 7 days post-tumor implantation at 1.25 mM/kg, sc for 5 days by histopathological analysis 18951804
BTI-TN-5B1-4 Function assay 30 mins Binding affinity to human CRBN (1 to 442 residues)/N-terminal 6His-tagged human DDB1 (1 to 1140 residues) expressed in baculovirus infected BTI-TN-5B1-4 insect cells after 30 mins by cy5 probe based fluorescence polarization assay, Kd=0.25μM 31117518
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Biological Activity

Description Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1.
Targets
E3 Ligase [6]
(Cell-free assay)		 TNF-alpha [2]
(Cell-free assay)
In vitro
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-p38 / p38 / Acetyl-H4 17620452
Immunofluorescence bFGF VCAM-1/CUL5 / NEDD8 25053990
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06146478 Completed
Transfusion-dependent Beta-Thalassemia
Blood Care Clinic|Khyber Medical University Peshawar
 January 25 2022 Phase 3
NCT04680195 Unknown status
Chronic Radiation Proctitis
Sixth Affiliated Hospital Sun Yat-sen University
 December 14 2020 Phase 2
NCT04469556 Active not recruiting
Pancreatic Cancer Metastatic|Pancreatic Ductal Adenocarcinoma|Advanced Pancreatic Cancer
University Health Network Toronto|Johns Hopkins University|Cold Spring Harbor Laboratory|Ontario Institute for Cancer Research|Dana-Farber Cancer Institute|Memorial Sloan Kettering Cancer Center|Stand Up To Cancer
 October 14 2020 Phase 2

Chemical Information & Solubility

Molecular Weight 258.23 Formula

C13H10N2O4
CAS No. 50-35-1 SDF Download Thalidomide SDF
Smiles C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 51 mg/mL ( (197.49 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

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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