• PROTAC은 특정 단백질의 분해를 유도하는 small molecule 입니다.
• 양옆으로 1)분해하려는 단백질에 붙는 Target protein ligand, 2)E3 Ligase에 붙는 E3 Ligase Ligand가 존재하고, 둘을 연결하는 3)Linker로 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.

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

 

Ligands
Cat No	Product Name / Activity
6356	AT 1
	(+)-JQ1 based PROTAC with selectivity for BRD4
6155	cis MZ 1
	Negative Control for MZ1
6416	CM 11New
	Homo-PROTAC for self-degradation of pVHL30
6417	CMP 98New
	Negative Control for CM 11
6327	dBET1
	(+)-JQ1 based PROTAC targeting BET bromodomains, active in vivo
6154	MZ 1
	(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells
6532	THAL SNS 032New
	Potent and selective CDK9 degrading PROTAC
6524	TL 12-186New
	Multikinase degrading PROTAC
6525	TL 13-27New
	Negative control for TL 12-186

 

Other
Cat No	Product Name / Activity
1956	Bestatin
	Aminopeptidase inhibitor
6157	cis VH 298
	Negative control for VH 298
6305	Lenalidomide
	Cereblon binder; induces ubiquitination and degradation of CK1a by E3 ubiquitin ligase
3984	Nutlin-3
	MDM2 antagonist; inhibits MDM2-p53 interaction
6075	Nutlin 3a
	MDM2 antagonist; active enantiomer of Nutlin-3 (Cat. No. 3984)
6302	Pomalidomide
	Cereblon ubiquitination inhibitor
0652	Thalidomide
	Binds cereblon, inhibiting ubiquitin ligase activity
6156	VH 298
	High-affinity inhibitor of VHL

  Tools for PROTAC R&D
 

Cat No	Product Name / Activity
6300	Azido-Thalidomide
	Azide-functionalized Thalidomide, 'click' ligand for PROTACs
6588	(+)-JQ1 carboxylic acidNew
	Carboxylic acid-functionalized BET bromodomain inhibitor
6589	(+)-JQ1 PANew
	'Click' target ligand for PROTACs; functionalized BET bromodomain inhibitor
6637	Pomalidomide - linker 1New
	Pomalidomide-PEG2-ethylamine
6466	TC E3 5031
	Carboxylic acid-functionalized Thalidomide, Cereblon ligand for PROTACs
6628	TC E3 5032New
	Precursor to Pomalidomide-based PROTACs
6467	Thalidomide - linker 1New
	Thalidomide-PEG3-ethylamine
6468	Thalidomide - linker 2New
	Thalidomide-PEG4-ethylamine
6469	Thalidomide - linker 3New
	Thalidomide-alkylC4-amine
6627	Thalidomide - linker 4New
	Thalidomide-alkylC6-amine
6463	VH 032 - linker 1New
	VH 032-PEG3-amine
6464	VH 032 - linker 2New
	VH 032-PEG4-amine
6465	VH 032 - linker 3New
	VH 032-alkylC4-amine
6462	VH 032, amine hydrochloride
	Functionalized VHL ligand for PROTACs