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 제품안내  신경약학   Pharmacology

프로탁 (PROTACs) for Targeted Protein Degradation (TPD)

프로탁 (PROTACs / PROteolysis TArgeting Chimeras)은 특정단백질의 분해를 유도하는 bi-valent bifunctional small molecule로, Ubiquitin-Proteasome system (UPS)를 이용하여 특정 질병 단백질을 분해하는 새로운 약물 작용 원리입니다.

TOCRIS는 특정 단백질을 타겟팅하는 Active Degrader와 Targeted Protein Degradation (TPD)의 연구를 돕기위한 Degrader Building Blocks을 제공합니다.

TOCRIS
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특징
  • PROTAC은 특정 단백질의 분해를 유도하는 system입니다.
  • 분해하려는 단백질에 붙는 Target protein ligand(1), E3 Ligase에 붙는 E3 Ligase Ligand(2) 부분과, 둘을 연결하는 Linker(3)로 구성됩니다.
  • 타겟 단백질에 대한 ligand 정보가 없을 경우, TAG degradation 방법을 이용합니다.
  • CRISPR/Cas9이나 RNA interference를 이용한 유전자 방법에 비해 사용이 간편하고, 처리량에 대한 optimization이 가능합니다.
  • PROTAC은 recycle 됩니다.
  • Tocris에서 제공하는 PROTAC은 모두 개발자의 license를 취득하여 제공되고 있습니다.
  • 많은 질병 관련 단백질을 약물 표적으로 이용함으로써 질병 치료제의 개발에 응용되고 있습니다.
  • 관심있는 ligand/linker에 쉽게 conjugation될 수 있도록 디자인되었습니다.
  • 잘 알려진 linker를 이용한 linker-functionalized E3 Ligase ligand를 제공합니다.
  • Custom design도 가능합니다.





  • 표적 단백질과 단백질 분해 촉진 효소인 E3 Ligase를 가깝게 연결해 주는 역할로 PROTAC이 작용합니다. PROTAC에 의해 연결이 되면, 표적단백질이 Ubiquitination되면서 Proteasome에 의해 degradation 됩니다.



  • 타겟 단백질에 대한 ligand 정보가 없을 경우, TAG을 fusion하여 이를 이용한 분해 기전을 이용합니다.
  • dTAG은 mutant FKBP12에, aTAG은 MTH1d에 specific한 knock-down을 유발합니다.



























  • PROTAC은 Degrader로서, 세포내에서 표적단백질을 분해할 수 있는 새로운 접근법입니다. 
  • 특정 단백질의 knockdown에 의한 downstream 효과를 조사하거나 특정 신호 전달 경로를 간섭하는데 이용됩니다. 

  Ligands
  Cat. No. Product Name / Activity
  6356 AT 1
    (+)-JQ1 based PROTAC with selectivity for BRD4
  6921 BSJ-03-123
    Selective Cdk6 degrader
  6938 BSJ-03-204
    Selective Cdk4/6 degrader
  6937 BSJ-04-132
    Selective Cdk4 degrader
  6416 CM 11
    Homo-PROTAC for self-degradation of pVHL30
  6948 CRBN-6-5-5-VHL
    Potent and selective cereblon degrader; cell-permeable
  6327 dBET1
    (+)-JQ1 based PROTAC targeting BET bromodomains, active in vivo
  6606 dBRD9
    Potent and selective BRD9 degrading PROTAC
  6607 dTRIM 24
    TRIM24 degrading PROTAC
  6154 MZ 1
    (+)-JQ1 based PROTAC that selectively degrades BRD4 in cells
  6532 THAL SNS 032
    Potent and selective Cdk9 degrading PROTAC
  6524 TL 12-186
    Multikinase degrading PROTAC
  6745 TL 13-112
    Selective ALK Degrader
  6744 TL 13-12
    Selective ALK degrader
  6936 VZ 185
    Potent and selective BRD7/9 Degrader
  6713 ZXH 3-26
    Potent and selective BRD4 degrader
     
  Controls
  Cat. No. Product Name / Activity
  6922 BSJ-Bump
    Negative control for BSJ-03-123 (Cat. No. 6921)
  6155 cis MZ 1
    Negative Control for MZ 1 (Cat. No. 6154)
  6939 cis-VZ 185
    Negative control for VZ 185 (Cat. No. 6936)
  6417 CMP 98
    Negative Control for CM 11 (Cat. No. 6416)
  6746 TL 13-110
    Negative control for TL 13-112 (Cat. No. 6745)
  6747 TL 13-22
    Negative control for TL 13-12 (Cat. No. 6744)
  6525 TL 13-27
    Negative control for TL 12-186 (Cat. No. 6524)

 

  • TOCRIS는 Degrader (PROTAC) 연구 지원을 위해 Building Block (E3 Ligase ligand와 linker)를 제공합니다.   
  Cereblon Targeting Ligands Plus Linkers
  Cat. No. Product Name / Activity
  6851 Pomalidomide 4'-alkylC2-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6682 Pomalidomide 4'-alkylC5-acid
    Cereblon ligand with alkyl linker and terminal acid for onward chemistry
  6716 Pomalidomide 4'-alkylC5-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6944 Pomalidomide 4'-alkylC8-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6637 Pomalidomide 4'-PEG2-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6681 Pomalidomide 4'-PEG3-acid
    Cereblon ligand with PEG linker and terminal acid for onward chemistry
  6963 Pomalidomide 4'-PEG4-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6946 Thalidomide 4'-oxyacetamide-alkylC8-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6850 Thalidomide 4'-ether-alkylC2-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6917 Thalidomide 4'-ether-alkylC4-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6627 Thalidomide 4'-ether-alkylC6-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6686 Thalidomide 4'-ether-PEG2-alkyne
    Cereblon ligand with PEG linker and terminal alkyne for onward chemistry
  6950 Thalidomide 4'-ether-PEG3-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6951 Thalidomide 4'-ether-PEG5-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6949 Thalidomide 4'-oxyacetamide-alkylC2-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6469 Thalidomide 4'-oxyacetamide-alkylC4-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6300 Thalidomide 4'-oxyacetamide-alkylC4-azide
    Cereblon ligand with alkyl linker and terminal azide for onward chemistry
  6968 Thalidomide 4'-oxyacetamide-alkylC6-amine
    Cereblon ligand with alkyl linker and terminal amine for onward chemistry
  6966 Thalidomide 4'-oxyacetamide-PEG1-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6967 Thalidomide 4'-oxyacetamide-PEG2-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6467 Thalidomide 4'-oxyacetamide-PEG3-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
  6468 Thalidomide 4'-oxyacetamide-PEG4-amine
    Cereblon ligand with PEG linker and terminal amine for onward chemistry
     
  VHL Targeting Ligands Plus Linkers
  Cat. No. Product Name / Activity
  6880 VH 032 amide-alkylC10-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6852 VH 032 amide-alkylC2-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6680 VH 032 amide-alkylC4-acid
    VHL ligand with alkyl linker and terminal acid for onward chemistry
  6465 VH 032 amide-alkylC4-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6985 VH 032 amide-alkylC5-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6853 VH 032 amide-alkylC6-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  7074 VH 032 amide-alkylC7-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6890 VH 032 amide-alkylC8-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6879 VH 032 amide-PEG1-amine
    VHL ligand with PEG linker and terminal amine for onward chemistry
  6684 VH 032 amide-PEG2-alkyne
    VHL ligand with PEG linker and terminal alkyne for onward chemistry
  6907 VH 032 amide-PEG2-amine
    VHL ligand with PEG linker and terminal amine for onward chemistry
  6679 VH 032 amide-PEG3-acid
    VHL ligand with PEG linker and terminal acid for onward chemistry
  6463 VH 032 amide-PEG3-amine
    VHL ligand with PEG linker and terminal amine for onward chemistry
  6464 VH 032 amide-PEG4-amine
    VHL ligand with PEG linker and terminal amine for onward chemistry
  6909 VH 032 phenol-alkylC4-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
  6910 VH 032 phenol-alkylC6-amine
    VHL ligand with alkyl linker and terminal amine for onward chemistry
     
  IAP Targeting Ligands Plus Linkers
  Cat. No. Product Name / Activity
  6474 A 410099.1 amide-alkylC4-amine
    A 410099.1 amide-alkylC4-amine
  6473 A 410099.1 amide-PEG2-amine
    A 410099.1 amide-PEG2-amine
  6472 A 410099.1 amide-PEG3-amine
    A 410099.1 amide-PEG3-amine

 

  Ligand
  • Linker에 붙일수 있는 E3 ligase ligand와 target 단백질에 대한 ligand입니다.
  Functionalized E3 Ligase Ligands
  Cat. No. Product Name / Activity
  6471 A 410099.1, amine
    Functionalized IAP ligand for PROTACs
  6466 TC E3 5031
    Carboxylic acid-functionalized Thalidomide; cereblon ligand for PROTACs
  6628 TC E3 5032
    Precursor to Pomalidomide-based PROTACs
  6685 Thalidomide, propargyl
    Alkyne-functionalized Thalidomide
  6462 VH 032, amine hydrochloride
    Functionalized VHL ligand for PROTACs
  6911 VH 032, phenol
    Hydroxyl functionalized VHL ligand
  6683 VH 032, propargyl
    Alkyne-functionalized VH 032
  6952 VH 101, phenol
    Hydroxyl functionalized VHL ligand
     
  Functionalized Warhead Ligands
  Cat. No. Product Name / Activity
  6588 (+)-JQ1 carboxylic acid
    Carboxylic acid-functionalized BET bromodomain inhibitor; target ligand for PROTACs
  6589 (+)-JQ1 PA
    Functionalized BET bromodomain inhibitor

 

  TAG Degradation Platform
  • aTAG, dTAG 시스템에 이용되는 Ligand 입니다.
  Ligands
  Cat. No. Product Name / Activity
  6970 aTAG 2139
    Degrader of MTH1 fusion proteins for use within the aTAG system
  6971 aTAG 4531
    Degrader of MTH1 fusion proteins for use within the aTAG system
  6605 dTAG-13
    Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
  6912 dTAG-7
    First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation










 

주문정보(Ordering Information)
CATNUM PRODUCT SIZE
6588(+)-JQ1 carboxylic acid25 mg
6589(+)-JQ1 PA25 mg
6471A 410099.1, amine100 mg
6356AT 15 mg
6970aTAG 21395 mg
6971aTAG 45315 mg
6300Azido-Thalidomide50 mg
6921BSJ-03-1235 mg
6938BSJ-03-2045 mg
6937BSJ-04-1325 mg
6922BSJ-Bump5 mg
6155cis MZ 15 mg
6939cis-VZ 1855 mg
6416CM 115 mg
6417CMP 985 mg
6948CRBN-6-5-5-VHL5 mg
6327dBET15 mg
6606dBRD95 mg
6605dTAG 135 mg
6912dTAG-75 mg
6607dTRIM 245 mg
6154MZ 15 mg
6637Pomalidomide - linker 125 mg
6681Pomalidomide - linker 225 mg
6682Pomalidomide - linker 325 mg
6716Pomalidomide - linker 425 mg
6851Pomalidomide - linker 725 mg
6963Pomalidomide - linker 825 mg
6944Pomalidomide 4'-alkylC8-amine25 mg
6466TC E3 5031100 mg
6628TC E3 5032100 mg
6532THAL SNS 0325 mg
6467Thalidomide - linker 125 mg
6949Thalidomide - linker 1025 mg
6950Thalidomide - linker 1125 mg
6951Thalidomide - linker 1225 mg
6966Thalidomide - linker 1325 mg
6967Thalidomide - linker 1425 mg
6968Thalidomide - linker 1525 mg
6468Thalidomide - linker 225 mg
6469Thalidomide - linker 325 mg
6627Thalidomide - linker 425 mg
6686Thalidomide - linker 525 mg
6850Thalidomide - linker 625 mg
6917Thalidomide - linker 925 mg
6946Thalidomide amide-alkylC8-amine25 mg
6685Thalidomide, propargyl50 mg
6524TL 12-1865 mg
6746TL 13-1105 mg
6745TL 13-1125 mg
6744TL 13-125 mg
6747TL 13-225 mg
6525TL 13-275 mg
6463VH 032 - linker 125 mg
6880VH 032 - linker 1025 mg
6890VH 032 - linker 1125 mg
6907VH 032 - linker 1225 mg
6985VH 032 - linker 1325 mg
6464VH 032 - linker 225 mg
6465VH 032 - linker 325 mg
6679VH 032 - linker 425 mg
6680VH 032 - linker 525 mg
6684VH 032 - linker 625 mg
6852VH 032 - linker 725 mg
6853VH 032 - linker 825 mg
6879VH 032 - linker 925 mg
7074VH 032 amide-alkylC7-amine25 mg
6909VH 032 phenol - linker 125 mg
6910VH 032 phenol - linker 225 mg
6462VH 032, amine hydrochloride100 mg
6911VH 032, phenol50 mg
6683VH 032, propargyl50 mg
6952VH 101, phenol50 mg
6936VZ 1855 mg
6713ZXH 3-265 mg