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시약 및 기기 상세
PROTAC 모니터링을 위한 SPRINTer™ Targeted Protein Degradation Cell-Based Assay Kit 이미지

PROTAC 모니터링을 위한 SPRINTer™ Targeted Protein Degradation Cell-Based Assay Kit

Eurofins DiscoverX의 SPRINTer™ Endogeneous Protein Turnover Biosensor Cell line은 disease-relevant cell model에 약물(예, PROTAC)을 처리하여 drug-induced protein turnover를 monitoring하기 위해 사용됩니다.

프린트 제품 문의

특징

 

  • SPRINTer™  (Sensing Protein Internal Turnover) Protein Turnover Biosensor assay 플랫폼은 PROTAC에 의해 유도되는 target 단백질의 분해를 정량하는데 이용됩니다.
  • Stable한 biosensor로 작용하는 cell line은 CRISPR/Cas9 기술을 이용하여 Enzyme Fragment Complementation (EFG) Enzyme Donor (ED)를 타겟 gene에 융합하여 ED-tagged target 단백질이 발현되도록 엔지니어링 되었습니다.
  • BRD4  혹은 c-Myc을 발현하는 colon cancer (HCT-116) cell과 blood cancer (K562) cell model을 제공합니다.
  • PROTAC에 의해 유도된 단백질의 분해와 합성 (protein turnover)를 모니터링 할 수 있습니다.
  • 타겟단백질의 turnover를 micro/nanomolar 수준으로 민감하게 측정할 수 있습니다.
  • 5시간 이내에 빠른 결과를 얻을 수 있으므로 효과적인 약물을 좀더 신속하게 판별할 수 있습니다.

 


원리

  • Sensor cell line은 ED가 tagging된 타겟 단백질을 발현하고, 여기에 PROTAC을 처리하면 이에 의해 타겟 단백질이 분해되므로 EFC 시그널이 소실됩니다. 즉, PROTAC에 의해 분해된 단백질의 양이 많을 수록 소실된 시그널이 많이 발생하는 원리입니다.




참고 데이터

  • Differentiate PROTAC Efficacies Using Different Cell Lines That Represent Disease-Relevant Cell Models



Select PROTACs display distinct efficacies among different cell types. A. SPRINTer HCT116 ED-BRD4 and B. SPRINTer K-562 ED-BRD4 cell lines were treated with BRD4 PROTACs (MZ1, dBET1, and JQ1-idasanutlin) for 5 hours and evaluated by EFC assay. Differences in rank order (and potency) of BRD4-targeted PROTACs that engage different E3 ligases were observed between the two cell types. JQ1-idasanutlin was shown to be more efficacious in the HCT-116 cell type compared to the K-562 cell type. C. Gene expression analysis reveals differential expression levels of MDM2 (which targets E3 ligase of JQ1-idasanutlin) between HCT116 and K-562 cell lines with lower expression seen in the K-562 cell line. This data suggests the abundance of the target E3 ligase in different cell lines is a key factor that influences the efficacy of JQ1-idasanutlin. Additionally, these results advise that it is important to choose a cell type with relevant expression of the E3 ligase that you are targeting. Note this same difference in potencies in K-562 to HCT116 cell lines also holds true for the equivalent c-myc cell lines (data available upon request). For comparison in the gene expression analysis, VHL and cereblon E3 ligases were also analyzed (noting VHL is the E3 ligase target for MZ1, and Cereblon is the E3 ligase target for dBET1), and POLR2A (RNA polymerase II subunit A) was used as a gene expression control. 



주문정보

주문정보 - Cat No, PRODUCT, SIZE, 수량 등 항목으로 구성되어있습니다.
  Product Cat.No. Size Maker Qty Data Sheet MSDS
SPRINTer™ Human BRAF(V600E) Targeted Protein Degradation Cell-Based Assay Kit (A375) 791-1008C057 kit EUROFINS DISCOVERX
SPRINTer™ Human BRD4 Targeted Protein Degradation Cell-Based Assay Kit (HCT-116) 791-1004C047 kit EUROFINS DISCOVERX
SPRINTer™ Human BRD4 Targeted Protein Degradation Cell-Based Assay Kit (K562) 791-1002C042 kit EUROFINS DISCOVERX
SPRINTer™ Human BTK Targeted Protein Degradation Cell-Based Assay Kit (K562) 791-1005C042 kit EUROFINS DISCOVERX
SPRINTer™ Human c-Myc Targeted Protein Degradation Cell-Based Assay Kit (HCT-116) 791-1003C047 kit EUROFINS DISCOVERX
SPRINTer™ Human c-Myc Targeted Protein Degradation Cell-Based Assay Kit (K562) 791-1001C042 kit EUROFINS DISCOVERX
SPRINTer™ Human CDKN1A (p21) Targeted Protein Degradation Cell-Based Assay Kit (HCT-116) 791-1006C047 kit EUROFINS DISCOVERX
SPRINTer™ Human IKZF1 Targeted Protein Degradation Cell-Based Assay Kit (K562) 791-1007C042 kit EUROFINS DISCOVERX
SPRINTer™ Human IKZF2 Targeted Protein Degradation Cell-Based Assay Kit (Jurkat) 791-1010C19 kit EUROFINS DISCOVERX
SPRINTer™ Human KRAS(G12C) Targeted Protein Degradation Cell-Based Assay Kit (A549) 791-1009C15 kit EUROFINS DISCOVERX
SPRINTer™ Human STAT3 Targeted Protein Degradation Cell-Based Assay Kit (A549) 791-1011C15 kit EUROFINS DISCOVERX
전체보기
Maker
EUROFINS DISCOVERX
Cat.No.
791-1008C057
Product
SPRINTer™ Human BRAF(V600E) Targeted Protein Degradation Cell-Based Assay Kit (A375)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1004C047
Product
SPRINTer™ Human BRD4 Targeted Protein Degradation Cell-Based Assay Kit (HCT-116)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1002C042
Product
SPRINTer™ Human BRD4 Targeted Protein Degradation Cell-Based Assay Kit (K562)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1005C042
Product
SPRINTer™ Human BTK Targeted Protein Degradation Cell-Based Assay Kit (K562)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1003C047
Product
SPRINTer™ Human c-Myc Targeted Protein Degradation Cell-Based Assay Kit (HCT-116)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1001C042
Product
SPRINTer™ Human c-Myc Targeted Protein Degradation Cell-Based Assay Kit (K562)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1006C047
Product
SPRINTer™ Human CDKN1A (p21) Targeted Protein Degradation Cell-Based Assay Kit (HCT-116)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1007C042
Product
SPRINTer™ Human IKZF1 Targeted Protein Degradation Cell-Based Assay Kit (K562)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1010C19
Product
SPRINTer™ Human IKZF2 Targeted Protein Degradation Cell-Based Assay Kit (Jurkat)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1009C15
Product
SPRINTer™ Human KRAS(G12C) Targeted Protein Degradation Cell-Based Assay Kit (A549)
Size
kit
Qty
Maker
EUROFINS DISCOVERX
Cat.No.
791-1011C15
Product
SPRINTer™ Human STAT3 Targeted Protein Degradation Cell-Based Assay Kit (A549)
Size
kit
Qty
전체보기

추천제품

관련제품

주문정보 - Cat No, PRODUCT, SIZE, 수량 등 항목으로 구성되어있습니다.
  Product Cat.No. Size Maker Qty Data Sheet MSDS

자료

  • 표적 단백질 분해 PRODUCT GUIDE

    표적 단백질 분해 PRODUCT GUIDE 이미지

    [TOCRIS]

    Targeted Protein Degradation에 대한 PRODUCT GUIDE 한글판 입니다.

  • Eurofins 신약개발 분석서비스

    Eurofins 신약개발 분석서비스 이미지

    [고마바이오텍]

    신약개발 과정에 필요한 분석 및 제작서비스가 수록된 종합 카탈로그입니다.

  • Targeted Protein Degradation Research Product Guide

    Targeted Protein Degradation Research Product Guide 이미지

    [TOCRIS]

    PROTAC 연구에 필요한 linker 및 degrader를 제공합니다.

  • Advance Emerging Therapeutics for Undruggable Targets

    Advance Emerging Therapeutics for Undruggable Targets 이미지

    [EUROFINS DISCOVERX]

    PROTAC을 이용한 Targeted Protein Degradation Drug Discovery Solutions을 안내합니다.

  • Targeted Protein Degradation Assays

    Targeted Protein Degradation Assays 이미지

    [EUROFINS DISCOVERX]

    PROTAC에 의해 유도된 Protein의 turnover를 측정하기 위한 assay platform에 대한 안내입니다.

웨비나/Video

  • [TOCRIS] Tools for Targeted Protein Degradation 이미지

    [TOCRIS] Tools for Targeted Protein Degradation

    PROTAC 기술에 대한 안내 영상입니다.

    동영상 보기
  • [TOCRIS] New Frontiers in Targeted Protein Degradation and Degrader Development 이미지

    [TOCRIS] New Frontiers in Targeted Protein Degradation and Degrader Development

    PROTAC 기술에 대한 안내입니다.

    동영상 보기
  • [EUROFINS DISCOVERY] Next-Generation Drug Discovery: Leveraging E3 Ligases for Targeted Protein Degradation 이미지

    [EUROFINS DISCOVERY] Next-Generation Drug Discovery: Leveraging E3 Ligases for Targeted Protein Degradation

    PROTAC 스크리닝에 대한 웨비나 입니다.

    동영상 보기
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제품 문의

 0.5 ml Elite Pre-stained Protein Ladder (2 x 0.25 ml) PAL-EPL-500 0.5ml 500
Maker
Cat.No.
Product
Size
Qty
Data Sheet
MSDS

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