• 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.
• 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.

  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
	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
	6605	dTAG-13
		Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
	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
	6713	ZXH 3-26
		Potent and selective BRD4 degrader
	Controls
	Cat. No.	Product Name / Activity
	6155	cis MZ 1
		Negative Control for MZ1
	6417	CMP 98
		Negative Control for CM 11
	6746	TL 13-110
		Negative control for TL 13-112
	6747	TL 13-22
		Negative control for TL 13-12
	6525	TL 13-27
		Negative control for TL 12-186

  TOCRIS는 Degrader (PROTAC) 연구 지원을 위해 Building Block (E3 Ligase ligand와 linker)를 제공합니다.   

	VHL Targeting Ligands Plus Linkers
	Cat. No.	Product Name	Linker Type	Number of Units	Example Chemistry
	6463	VH 032 - linker 1	PEG	3	Amine
	6464	VH 032 - linker 2	PEG	4	Amine
	6465	VH 032 - linker 3	Alkyl	4	Amine
	6679	VH 032 - linker 4	PEG	3	CH2CH2COOH
	6680	VH 032 - linker 5	Alkyl	4	Carboxylic Acid
	6684	VH 032 - linker 6	PEG	2	Alkyne
	6852	VH 032 - linker 7	Alkyl	2	Amine
	6853	VH 032 - linker 8	Alkyl	6	Amine
	6879	VH 032 - linker 9	PEG	1	Amine
	6880	VH 032 - linker 10	Alkyl	10	Amine
	6890	VH 032 - linker 11	Alkyl	8	Amine
	6907	VH 032 - linker 12	PEG	2	Amine
	Cereblon Targeting Ligands Plus Linkers
	Cat. No.	Product Name	Linker Type	Number of Units	Conjugation Functionality
	6637	Pomalidomide - linker 1	PEG	2	Amine
	6681	Pomalidomide - linker 2	PEG	3	Carboxylic Acid
	6682	Pomalidomide - linker 3	Alkyl	5	Carboxylic Acid
	6716	Pomalidomide - linker 4	Alkyl	5	Amine
	6851	Pomalidomide - linker 7	Alkyl	2	Amine
	6963	Pomalidomide - linker 8	PEG	4	Ethylamine
	6467	Thalidomide - linker 1	PEG	3	Amine
	6468	Thalidomide - linker 2	PEG	4	Amine
	6469	Thalidomide - linker 3	Alkyl	4	Amine
	6627	Thalidomide - linker 4	Alkyl	6	Amine
	6686	Thalidomide - linker 5	PEG	2	Alkyne
	6850	Thalidomide - linker 6	Alkyl	2	Amine
	6917	Thalidomide - linker 9	Alkyl	4	Amine
	6949	Thalidomide - linker 10	Alkyl	2	Amine
	6951	Thalidomide - linker 12	PEG	5	Ethylamine
	6966	Thalidomide - linker 13	PEG	1	Ethylamine
	6967	Thalidomide - linker 14	PEG	2	Ethylamine
	6968	Thalidomide - linker 15	Alkyl	6	Amine
	6300	Azido-Thalidomide	Alkyl	4	Azide
	Functionalized E3 Ligase Ligands
	Cat. No.	Product Name	Target E3	Reactive Handle	Reaction Chemistry
	6466	TC E3 5031	Cereblon	Carboxylic acid	Amide coupling
	6628	TC E3 5032	Cereblon	Fluorine	Nucleophilic aromatic substitution
	6685	Thalidomide, propargyl	Cereblon	Alkyne	Click chemistry
	6462	VH 032, amine hydrochloride	VHL	Primary amine	Amide coupling
	6683	VH 032, propargyl	VHL	Alkyne	Click chemistry
	Functionalized Warhead Ligands
	Cat. No.	Product Name	Target Protein	Reactive Handle	Reaction Chemistry
	6588	(+)-JQ1 carboxylic acid	BET Bromodomains	Carboxylic acid	Amide coupling
	6589	(+)-JQ1 PA	BET Bromodomains	Alkyne	Click chemistry

• Targeted Protein Degradation Research Product Guide
• Targeted Protein Degradation Poster