Thalidomide (K17)

Catalog No.S1193

For research use only.

Thalidomide (K17) 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.

Thalidomide (K17) Chemical Structure

CAS No. 50-35-1

Selleck's Thalidomide (K17) has been cited by 29 publications

Purity & Quality Control

Choose Selective E3 ligase Ligand Inhibitors

Biological Activity

Description Thalidomide (K17) 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 M13uVmZ2dmO2aX;uJIF{e2G7 NEDFWVJKdmirYnn0bY9vKG:oIFnMMVEu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBqdiCKZVzhJINmdGy|IHHzd4V{e2WmIHHzJIJtd2OtaX7nJI9nKHB3MD;wOlUhdnWlbHXhdkB1emGwc3zvZ4F1cW:wLDDJR|UxRTJwMEVOwG0> Mn7CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd6NEW4OVAoRjF5OES1PFUxRC:jPh?=
RAW264.7 MoTvRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>? NH:ybYsyOCC3TR?= M1;ZWlMhcHK| Mn;mRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDpckBud3W|ZTDMVHMu[WO2aY\heIVlKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KFKRUzDzZ4F3\W6paX7nJIFkfGm4aYT5JIF1KDFyIIXNJJBz\XS{ZXH0[YQh\m:{IEOgbJJ{KGKnZn;y[UBNWFNiY3jhcIxmdmenIH3lZZN2emWmIHL5JIRm[3KnYYPlJIlvKG[udX;y[ZNk\W62IHnueIVve2m2eTDifUBkd26ob3PhcEBucWO{b4Pjc5B6 NWXtSYk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3NlM{PTdpPkG4O|I{OzV5PD;hQi=>
RAW264.7 MVXGeY5kfGmxbjDhd5NigQ>? NYfFOmlNOSC3TR?= NIDOT4s{KGi{cx?= M3XJ[XJm\HWldHnvckBqdiCrTl;TJIV5eHKnc4Ppc44hcW5iTGDTMYFkfGm4YYTl[EBud3W|ZTDSRXczPjRwNzDj[YxteyCjdDCxJJVOKHC{ZYTy[YF1\WRiZn;yJFMhcHK|IHLl[o9z\SCOUGOgZ4hidGynbnflJIF{e2W|c3XkJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Q> Mn3pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5MkOzOVcoRjF6N{KzN|U4RC:jPh?=
RAW264.7 MlflSpVv[3Srb36gZZN{[Xl? NVfPdll1OTBidV2= MmDaN{BpenN? Mn\jVoVlfWO2aX;uJIlvKGmQT2Og[ZhxemW|c3nvckBqdiCOUGOtZYN1cX[jdHXkJI1wfXOnIGLBW|I3PC55IHPlcIx{KGG2IEGwJJVOKHC{ZYTy[YF1\WRiZn;yJFMhcHK|IHLl[o9z\SCOUGOgZ4hidGynbnflJIF{e2W|c3XkJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Q> NV7SW21uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3NlM{PTdpPkG4O|I{OzV5PD;hQi=>
RAW264.7 M{jzbGZ2dmO2aX;uJIF{e2G7 NGLBbIcyOCC3TR?= MlH5N{BpenN? NF3ibJlT\WS3Y4Tpc44hcW5icFXST|EwOiCneIDy[ZN{cW:wIHnuJGxRWy2jY4TpeoF1\WRibX;1d4UhWkGZMk[0Mlch[2WubIOgZZQhOTBidV2gdJJmfHKnYYTl[EBnd3JiMzDodpMh[mWob4LlJGxRWyClaHHscIVv\2ViYYPz[ZN{\WRiYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdB?= M2T5N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6N{KzN|U4Lz5zOEeyN|M2PzxxYU6=
Ehrlich ascites carcinoma cells NUHEVYRNXG:6aXPpeJkh[XO|YYm= Mk\mNU4zPSCvTT;r[y=> NUnXWYg2PyCmYYnz MYLUc5hq[2m2eTDpckBUf2m|czDhcIJqdm9ibX;1d4Uh[mWjcnnu[{Bud3W|ZTDFbJJtcWOqIHHzZ4l1\XNiY3HyZ4lvd22jIHPlcIx{KGG|c3Xzd4VlKGG|IH\vZ4FtKGSnZ3Xu[ZJifGmxbjDv[kBp\XCjdH;jfZRmeyC2cnXheIVlKGGodHXyJFch\GG7czDwc5N1NXS3bX;yJIlueGyjboTheIlwdiCjdDCxMlI2KG2PL3vnMEB{[yCob4KgOUBl[Xm|IHL5JIhqe3SxcHH0bI9td2erY3HsJIFv[Wy7c3nz M3XyRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUWxPFA1Lz5zOEm1NVgxPDxxYU6=
Ehrlich ascites carcinoma cells Mo\TWI95cWOrdImgZZN{[Xl? M1HuOVEvOjVibV2vb4c> NV\PPYVZPyCmYYnz MXLUc5hq[2m2eTDpckBUf2m|czDhcIJqdm9ibX;1d4Uh[mWjcnnu[{Bud3W|ZTDFbJJtcWOqIHHzZ4l1\XNiY3HyZ4lvd22jIHPlcIx{KGG|c3Xzd4VlKGG|IH\vZ4FtKG6nY4Lvd4l{KG:oIHjldIF1d2O7dHXzJJRz\WG2ZXSgZYZ1\XJiNzDkZZl{KHCxc4SteJVud3JiaX3wcIFvfGG2aX;uJIF1KDFwMkWgcW0wc2duIIPjJIZweiB3IHThfZMh[nliaHnzeI9x[XSqb3zv[4lk[WxiYX7hcJl{cXN? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl3MUiwOEc,OTh7NUG4NFQ9N2F-
BTI-TN-5B1-4 MXzGeY5kfGmxbjDhd5NigQ>? MYCzNEBucW6| M1fJVmJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gR3JDViBqMTD0c{A1PDJicnXzbYR2\XNrL16teIVzdWmwYXygOmhqey22YXfn[YQhcHWvYX6gSGRDOSBqMTD0c{AyOTRyIILld4llfWW|KTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiQmTJMXRPNTWEMT20JIlve2WldDDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KGO7NTDwdo9j\SCkYYPl[EBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDL[F0xNjJ3zszN NIXoNXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUGxO|UyQCd-M{GxNVc2OTh:L3G+
Assay
Methods Test Index PMID
Western blot p-p38 / p38 / Acetyl-H4 17620452
Immunofluorescence bFGF ; VCAM-1/CUL5 / NEDD8 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]

Protocol (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 258.23
Formula

C13H10N2O4

CAS No. 50-35-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(=O)NC(=O)C1N2C(=O)C3=CC=CC=C3C2=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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