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 Á¦Ç°¾È³»  ºÐ¼® Á¦ÀÛ ¼­ºñ½º   ½Å¾à°³¹ß Ž»ö ¼­ºñ½º  PROTAC

E3scan¢â Ligand Binding Assay ¼­ºñ½º

Target Protein Degradation (PROTAC) ¿¬±¸¸¦ À§ÇÑ E3 ligase ligand binding assay ¼­ºñ½º¸¦ Á¦°øÇÕ´Ï´Ù.

Eurofins Discovery
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  • Å×½ºÆ® compound¿Í E3 ligase°£ÀÇ »óÈ£ÀÛ¿ë¿¡ ÀÇÇÑ binding affinity¸¦ Á¤·®ÇØ µå¸³´Ï´Ù.
  • KINOMEscan® technology¸¦ ±â¹ÝÀ¸·Î ÇÏ¿©, DNA-tagged target protein°ú high sensitivity qPCR readoutÀ» ÅëÇØ ¹Î°¨Çϰí Á¤È®ÇÑ ligand KDs¸¦ ÃøÁ¤ÇÕ´Ï´Ù.
  • ³·Àº picomolar ¹üÀ§±îÁöµµ ÃøÁ¤µË´Ï´Ù. 
  • Ä¡·áÁ¦·Î¼­ÀÇ °¡´É¼º°ú ÀáÀçÀûÀÎ off-target liability¿¡ ´ëÇÑ Á¤º¸¸¦ ¾òÀ» ¼ö ÀÖ½À´Ï´Ù.
  • ºÐ¼® °¡´ÉÇÑ E3 ligase ligand Ÿ°Ù ±×·ì : VHL, MDM2, MDM4, CRBN, cIAP1, cIAP2 and XIAP (all full length)


  • DNA taggingµÈ E3 ligase¿Í solid support¿¡ °íÁ¤µÈ known E3 ligase ligandÀÇ binding Á¤µµ¸¦ ÃøÁ¤. test compound°¡ µÎ ¹ÝÀÀ »çÀÌ¿¡¼­ competitionÀ» °¡Áú °æ¿ì °íÁ¤È­µÈ solid support¿¡ ÀÇÇØ ÃøÁ¤µÇ´Â DNAÀÇ ¾çÀº °¨¼ÒµÊ.



  • Representative data of MDM2 validation with two MDM2 Inhibitors Idasanutlin (Kd 1.3 nM) and Nutlin 3a (Kd 75.8 nM) and CRBN with CRBN inhibitors Thalidomide (Kd 23 nM) and Lenalidomide (Kd 28 nM).