[TOCRIS] 표적단백질 분해기술 | PROTAC® Degraders & Linkers

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[TOCRIS] 표적단백질 분해기술 | PROTAC® Degraders & Linkers

Maker : TOCRIS

PROTAC은 특정단백질의 분해를 유도하는 bi-valent bifunctional small molecule로, Ubiquitin-Proteasome system (UPS)를 이용하여 특정 질병 단백질을 분해하는 새로운 약물 작용 원리입니다. PROTAC 연구에 이용되는 linker, degrader를 소개합니다.

프린트 제품 문의

특징

PROTAC은 특정 표적 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.
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.

원리

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

주요 제품

1. Protein Degraders (단백질 분해 유도제)

단백질 분해 유도제(예: PROTAC® 분자, SNIPER 등)는 세포 내 표적 단백질을 제거(knockdown)하기 위한 새로운 접근법입니다. E3 유비퀴틴 리가아제(E3 ubiquitin ligase)에 결합하는 부위와 표적 단백질에 결합하는 부위가 링커(linker)로 연결된 이 하이브리드(결합) 분자는, 세포 내 단백질 분해 시스템(프로테아좀)을 유도하여 특정 표적 단백질을 선택적으로 분해합니다. 이러한 방식은 단백질 제거에 따른 하위 신호 전달 체계의 영향을 연구하거나, 특정 신호 경로를 차단하는 데 사용될 수 있습니다.

Bromodomain (BRD)		Cyclin Dependent Kinase (CDK)		CBP and p300
Cat. No.	Product	Cat. No.	Product	Cat. No.	Product
7256	ARV 771	6921	BSJ-03-123	7682	JQAD1
6356	AT 1	6938	BSJ-03-204
6327	dBET1	7528	BSJ-4-116	E3 Ligase
6945	dBET6	7800	CPS2	Cat. No.	Product
6606	dBRD9	7940	HEMTAC 26	6416	CM 11
6943	dBRD9-A	7304	JH-XI-10-02	7219	CRBN PROTAC® 14a
7828	HHP 9	7813	LL-K9-3	6948	CRBN-6-5-5-VHL
8152	JQ dS-4	8076	MS 28	8021	CST 626
6154	MZ 1	6532	THAL SNS 032	6607	dTRIM 24
7432	SIM1
6936	VZ 185

Histone Deacetylase (HDAC)		Polycomb Repressive Complex (PRC)		Kinase
Cat. No.	Product	Cat. No.	Product	Cat. No.	Product
8024	CT-4	8077	MS 147	7427	CG 858
7882	HDAC4 CHDI Degrader 11	7816	UNC 6852	7160	DD 03-171
8083	JPS016			7306	FC 11
8085	JPS036	Receptor Degraders		7265	GMB 475
		Cat. No.	Product	7818	GSK 215
MAPK		7254	ARCC 4	7983	IRAK3 Degrader 23
Cat. No.	Product	7258	Gefitinib-based PROTAC® 3	7837	JB 300
7177	NR 7h	7886	HER2 PROTAC® CH7C4	8029	JNJ 1013
7268	SJFα	7395	MS 154	8081	MS 143
7267	SJFδ	7397	MS 39	8951	NX 2127
		7261	SJF 1521	8856	NX 5948
Raf and Ras		7262	SJF 1528	8116	PPM-3
Cat. No.	Product	7266	SJF 8240	7651	PT-65
7425	CG 428	7120	SNIPER(ER)-87	7675	SJ 1008030
7427	CG 858	7278	α1A-AR Degrader 9c	7727	SJ 10542
7745	CST 905			7721	SJ 11646
7420	LC 2			7259	TBK1 PROTAC® 3i
7463	SJF 0628			6524	TL 12-186
				6745	TL 13-112
				6744	TL 13-12
				7240	ZNL 02-096

2. Degrader Building Blocks

단백질 분해 블록은 연구자가 원하는 리간드나 링커에 쉽게 결합(conjugation)할 수 있도록 기능성 핸들(functional handles)이 부착되어 있습니다. 당사의 제품군에는 결합 친화도(binding affinity)를 저해하지 않는 것으로 검증된 위치에 기능기가 도입된, 가장 효과적이고 널리 사용되는 E3 유비퀴틴 리가아제 리간드들이 포함되어 있습니다. 또한, 일반적인 링커 그룹과 결합된 형태의 E3 리가아제 리간드도 함께 공급합니다.

Degrader Building Block은 Reactive handle을 포함한 linker에 E3 ligase ligand가 붙은 형태로, E3 ligase ligand (CRBN, VHL, IAP), exit vector 유형 및 위치, linker의 길이와 유형 등을 스크리닝하는데 유용합니다.

Cereblon Targeting Ligands Plus Linkers
Cat. No.	Product	Cat. No.	Product
7516	Lenalidomide 4'-alkylC3-azide	7436	Pomalidomide 4'-PEG4-azide
7517	Lenalidomide 4'-alkylC5-azide	7095	Pomalidomide 4'-PEG5-acid
7075	Lenalidomide 4'-PEG1-amine	7924	Pomalidomide 4'-PEG5-amine
7513	Lenalidomide 4'-PEG1-azide	7437	Pomalidomide 4'-PEG5-azide
7093	Lenalidomide 4'-PEG2-amine	7470	Pomalidomide 5'-fluoro-6'-piperazine
7514	Lenalidomide 4'-PEG2-azide	7471	Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine
7076	Lenalidomide 4'-PEG3-amine	7468	Pomalidomide 5'-piperazine
7677	Lenalidomide 5'-amine	7469	Pomalidomide 5'-piperazine-4-methylpiperidine
7472	Lenalidomide 5'-piperazine	7913	Pomalidomide 5'-piperidine-acid
7473	Lenalidomide 5'-piperazine-4-methylpiperidine	7329	Thalidomide 4'-ether-alkylC2-acid
8848	Lenalidomide 5'-piperazine-7'-methoxy	6850	Thalidomide 4'-ether-alkylC2-amine
7994	PAG 3'-fluoro-4'-piperazine	7330	Thalidomide 4'-ether-alkylC3-acid
7996	PAG 3'-piperazine	7521	Thalidomide 4'-ether-alkylC3-azide
7997	PAG 3'-piperazine-4-methylpiperidine	7331	Thalidomide 4'-ether-alkylC4-acid
7998	PAG 4'-piperazine	6917	Thalidomide 4'-ether-alkylC4-amine
7999	PAG 4'-piperazine-4-methylpiperidine	7332	Thalidomide 4'-ether-alkylC5-acid
7732	Pomalidomide 4'-alkylC10-amine	7522	Thalidomide 4'-ether-alkylC5-azide
6851	Pomalidomide 4'-alkylC2-amine	7333	Thalidomide 4'-ether-alkylC6-acid
7439	Pomalidomide 4'-alkylC2-azide	6627	Thalidomide 4'-ether-alkylC6-amine
7096	Pomalidomide 4'-alkylC3-acid	7829	Thalidomide 4'-ether-alkylC6-azide
7205	Pomalidomide 4'-alkylC3-amine	7334	Thalidomide 4'-ether-alkylC7-acid
7440	Pomalidomide 4'-alkylC3-azide	7335	Thalidomide 4'-ether-alkylC8-acid
7209	Pomalidomide 4'-alkylC4-acid	7403	Thalidomide 4'-ether-alkylC8-amine
7441	Pomalidomide 4'-alkylC4-azide	7518	Thalidomide 4'-ether-PEG1-azide
6682	Pomalidomide 4'-alkylC5-acid	6686	Thalidomide 4'-ether-PEG2-alkyne
6716	Pomalidomide 4'-alkylC5-amine	7519	Thalidomide 4'-ether-PEG2-azide
7442	Pomalidomide 4'-alkylC5-azide	6950	Thalidomide 4'-ether-PEG3-amine
7210	Pomalidomide 4'-alkylC6-acid	7520	Thalidomide 4'-ether-PEG3-azide
7923	Pomalidomide 4'-alkylC6-amine	6951	Thalidomide 4'-ether-PEG5-amine
7443	Pomalidomide 4'-alkylC6-azide	6913	Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine
7097	Pomalidomide 4'-alkylC7-acid	6949	Thalidomide 4'-oxyacetamide-alkylC2-amine
7208	Pomalidomide 4'-alkylC7-amine	6300	Thalidomide 4'-oxyacetamide-alkylC4-azide
7211	Pomalidomide 4'-alkylC8-acid	6968	Thalidomide 4'-oxyacetamide-alkylC6-amine
6944	Pomalidomide 4'-alkylC8-amine	6946	Thalidomide 4'-oxyacetamide-alkylC8-amine
7094	Pomalidomide 4'-PEG1-acid	6966	Thalidomide 4'-oxyacetamide-PEG1-amine
7203	Pomalidomide 4'-PEG1-amine	6967	Thalidomide 4'-oxyacetamide-PEG2-amine
7434	Pomalidomide 4'-PEG1-azide	6467	Thalidomide 4'-oxyacetamide-PEG3-amine
7212	Pomalidomide 4'-PEG2-acid	7733	Thalidomide 5'-amine-alkylC10-amine
6637	Pomalidomide 4'-PEG2-amine	7988	Thalidomide 5'-amine-alkylC6-amine
7307	Pomalidomide 4'-PEG2-azide	7557	Thalidomide 5'-amine-alkylC8-amine
7204	Pomalidomide 4'-PEG3-amine	7735	Thalidomide 5'-amine-PEG1-amine
7435	Pomalidomide 4'-PEG3-azide	7736	Thalidomide 5'-amine-PEG2-amine
7213	Pomalidomide 4'-PEG4-acid	7737	Thalidomide 5'-amine-PEG3-amine
6963	Pomalidomide 4'-PEG4-amine

IAP Targeting Ligands Plus Linkers
Cat. No.	Product	Cat. No.	Product
6472	A 410099.1 amide-PEG3-amine	7220	A 410099.1 amide-PEG4-amine
6473	A 410099.1 amide-PEG2-amine	7221	A 410099.1 amide-PEG5-amine
6474	A 410099.1 amide-alkylC4-amine

VHL Targeting Ligands Plus Linkers
Cat. No.	Product	Cat. No.	Product
6880	VH 032 amide-alkylC10-amine	7404	VH 032 amide-alkylC9-acid
7106	VH 032 amide-alkylC2-acid	7566	VH 032 amide-alkylC9-amine
6852	VH 032 amide-alkylC2-amine	7104	VH 032 amide-PEG1-acid
7216	VH 032 amide-alkylC3-acid	6879	VH 032 amide-PEG1-amine
7073	VH 032 amide-alkylC3-amine	7214	VH 032 amide-PEG2-acid
6680	VH 032 amide-alkylC4-acid	6907	VH 032 amide-PEG2-amine
6465	VH 032 amide-alkylC4-amine	6463	VH 032 amide-PEG3-amine
7217	VH 032 amide-alkylC5-acid	8123	VH 032 amide-PEG3-BCN
6985	VH 032 amide-alkylC5-amine	7215	VH 032 amide-PEG4-acid
7867	VH 032 amide-alkylC5-azide	6464	VH 032 amide-PEG4-amine
7107	VH 032 amide-alkylC6-acid	7105	VH 032 amide-PEG5-acid
6853	VH 032 amide-alkylC6-amine	7568	VH 032 amide-PEG6-amine
7925	VH 032 amide-alkylC7-acid	6909	VH 032 phenol-alkylC4-amine
7074	VH 032 amide-alkylC7-amine	6910	VH 032 phenol-alkylC6-amine
7108	VH 032 amide-alkylC8-acid	7293	VH 101 phenol-alkylC4-amine
6890	VH 032 amide-alkylC8-amine	7294	VH 101 phenol-alkylC6-amine

Functionalized E3 Ligase Ligands
Cat. No.	Product	Cat. No.	Product
7678	5-Amino-Thalidomide	6685	Thalidomide, propargyl
6471	A 410099.1, amine	6466	Thalidomide-4-hydroxyacetate
8066	CST 530, Phenol	7759	UNC 1215, acid
7178	LCL 161, phenol	6462	VH 032, amine
7634	Me VH 032, amine	6911	VH 032, phenol
7858	PD 4'-oxyacetic acid	6683	VH 032, propargyl
7859	PD 4'-piperazine	7861	VH 032, thiol
7670	Phenyl-glutarimide 4'-oxyacetic acid	7758	VH 101, acid
7729	Phenyl-glutarimide 4'-piperazine	6952	VH 101, phenol
7773	tDHU, acid	7884	VH 101, thiol
7456	Thalidomide, 5'-fluoro	8075	VHF 543, amine

Functionalized Warhead Ligands
Cat. No.	Product	Cat. No.	Product
7689	(+)-JQ1 bump, acid functionalized	7576	(+)-JQ1 maleimide

LYTAC Building Blocks
Cat. No.	Product	Cat. No.	Product
7635	tri-GalNAc biotin	8015	tri-GalNAc-PEG3-Azide
7401	tri-GalNAc COOH	7780	β-GalNAc-PEG4-Azide
7781	tri-GalNAc-C5-amine

VHL Targeting Ligands Plus Linkers

Cat. No.	Product Name	Linker Type	Number of Units	Conjugation Functionality
7106	VH 032 amide-alkylC2-acid	Alkyl	2	Carboxylic Acid
6852	VH 032 amide-alkylC2-amine	Alkyl	2	Amine
7216	VH 032 amide-alkylC3-acid	Alkyl	3	Acid
7073	VH 032 amide-alkylC3-amine	Alkyl	3	Amine
6680	VH 032 amide-alkylC4-acid	Alkyl	4	Carboxylic Acid
6465	VH 032 amide-alkylC4-amine	Alkyl	4	Amine
7217	VH 032 amide-alkylC5-acid	Alkyl	5	Acid
6985	VH 032 amide-alkylC5-amine	Alkyl	5	Amine
7867	VH 032 amide-alkylC5-azide	Alkyl	5	Azide
7107	VH 032 amide-alkylC6-acid	Alkyl	6	Carboxylic Acid
6853	VH 032 amide-alkylC6-amine	Alkyl	6	Amine
7925	VH 032 amide-alkylC7-acid	Alkyl	7	Carboxylic Acid
7074	VH 032 amide-alkylC7-amine	Alkyl	7	Amine
7108	VH 032 amide-alkylC8-acid	Alkyl	8	Carboxylic Acid
6890	VH 032 amide-alkylC8-amine	Alkyl	8	Amine
7404	VH 032 amide-alkylC9-acid	Alkyl	9	Carboxylic Acid
7566	VH 032 amide-alkylC9-amine	Alkyl	9	Amine
6880	VH 032 amide-alkylC10-amine	Alkyl	10	Amine
7104	VH 032 amide-PEG1-acid	PEG	1	Acid
6879	VH 032 amide-PEG1-amine	PEG	1	Amine
6907	VH 032 amide-PEG2-amine	PEG	2	Amine
6684	VH 032 amide-PEG2-alkyne	PEG	2	Alkyne
6679	VH 032 amide-PEG3-acid	PEG	3	Carboxylic Acid
6463	VH 032 amide-PEG3-amine	PEG	3	Amine
7215	VH 032 amide-PEG4-acid	PEG	4	Carboxylic Acid
6464	VH 032 amide-PEG4-amine	PEG	4	Amine
7105	VH 032 amide-PEG5-acid	PEG	5	Acid
7568	VH 032 amide-PEG6-amine	PEG	6	Amine
6909	VH 032 phenol-alkylC4-amine	Alkyl	4	Amine
6910	VH 032 phenol-alkylC6-amine	Alkyl	6	Amine
7293	VH 101 phenol-alkylC4-amine	Alkyl	4	Amine

Cereblon Targeting Ligands Plus Linkers

Cat. No.	Product Name	E3 Ligase Exit Vector	Linker Type	Number of Units	Conjugation Functionality
7516	Lenalidomide 4'-alkylC3-azide	-	alkyl	3	Azide
7517	Lenalidomide 4'-alkylC5-azide	-	alkyl	5	Azide
7075	Lenalidomide 4'-PEG1-amine	-	PEG	1	Amine
7513	Lenalidomide 4'-PEG1-azide	-	PEG	1	Azide
7093	Lenalidomide 4'-PEG2-amine	-	PEG	2	Amine
7514	Lenalidomide 4'-PEG2-azide	-	PEG	2	Azide
7076	Lenalidomide 4'-PEG3-amine	-	PEG	3	Amine
7515	Lenalidomide 4'-PEG3-azide	-	PEG	3	Azide
7472	Lenalidomide 5'-piperazine	Piperazine	-	-	Amine
7473	Lenalidomide 5'-piperazine-4-methylpiperidine	Piperazine	Methyl-piperidine	1	Amine
7998	PAG 4'-piperazine	Piperazine	-	-	Amine
7999	PAG 4'-piperazine-4-methylpiperidine	Piperazine	Methyl-piperidine	1	Amine
6851	Pomalidomide 4'-alkylC2-amine	-	Alkyl	2	Amine
7439	Pomalidomide 4'-alkylC2-azide	-	Alkyl	2	Azide
7096	Pomalidomide 4'-alkylC3-acid	-	Alkyl	3	Carboxylic Acid
7205	Pomalidomide 4'-alkylC3-amine	-	Alkyl	3	Amine
7440	Pomalidomide 4'-alkylC3-azide	-	Alkyl	3	Azide
7209	Pomalidomide 4'-alkylC4-acid	-	Alkyl	4	Carboxylic Acid
7441	Pomalidomide 4'-alkylC4-azide	-	Alkyl	4	Azide
6682	Pomalidomide 4'-alkylC5-acid	-	Alkyl	5	Carboxylic Acid
6716	Pomalidomide 4'-alkylC5-amine	-	Alkyl	5	Amine
7442	Pomalidomide 4'-alkylC5-azide	-	Alkyl	5	Azide
7210	Pomalidomide 4'-alkylC6-acid	-	Alkyl	6	Carboxylic Acid
7923	Pomalidomide 4'-alkylC6-amine	-	Alkyl	6	Amine
7443	Pomalidomide 4'-alkylC6-azide	-	Alkyl	6	Azide
7097	Pomalidomide 4'-alkylC7-acid	-	Alkyl	7	Carboxylic Acid
7208	Pomalidomide 4'-alkylC7-amine	-	Alkyl	7	Amine
7211	Pomalidomide 4'-alkylC8-acid	-	Alkyl	8	Carboxylic Acid
6944	Pomalidomide 4'-alkylC8-amine	-	Alkyl	8	Amine
7732	Pomalidomide 4'-alkylC10-amine	-	Alkyl	10	Amine
7094	Pomalidomide 4'-PEG1-acid	-	PEG	1	Acid
7203	Pomalidomide 4'-PEG1-amine	-	PEG	1	Ethylamine
7434	Pomalidomide 4'-PEG1-azide	-	PEG	1	Azide
7212	Pomalidomide 4'-PEG2-acid	-	PEG	2	Acid
6637	Pomalidomide 4'-PEG2-amine	-	PEG	2	Amine
7307	Pomalidomide 4'-PEG2-azide	-	PEG	2	Azide
6681	Pomalidomide 4'-PEG3-acid	-	PEG	3	Carboxylic Acid
7204	Pomalidomide 4'-PEG3-amine	-	PEG	3	Ethylamine
7435	Pomalidomide 4'-PEG3-azide	-	PEG	3	Azide
7213	Pomalidomide 4'-PEG4-acid	-	PEG	4	Acid
6963	Pomalidomide 4'-PEG4-amine	-	PEG	4	Ethylamine
7436	Pomalidomide 4'-PEG4-azide	-	PEG	4	Azide
7095	Pomalidomide 4'-PEG5-acid	-	PEG	5	Acid
7437	Pomalidomide 4'-PEG5-azide	-	PEG	5	Azide
7438	Pomalidomide 4'-PEG6-azide	-	PEG	6	Azide
7468	Pomalidomide 5'-piperazine	Piperazine	-	-	Amine
7469	Pomalidomide 5'-piperazine-4-methylpiperidine	Piperazine	Methyl-piperidine	1	Amine
7470	Pomalidomide 5'-fluoro-6-piperazine	Piperazine	-	-	Amine
7471	Pomalidomide 5'-fluoro-6-piperazine-4-methylpiperidine	Piperazine	Methyl-piperidine	1	Amine
7329	Thalidomide 4'-ether-alkylC2-acid		Alkyl	2	Acid
6850	Thalidomide 4'-ether-alkylC2-amine		Alkyl	2	Amine
7330	Thalidomide 4'-ether-alkylC3-acid		Alkyl	3	Acid
7521	Thalidomide 4'-ether-alkylC3-azide		Alkyl	3	Azide
7331	Thalidomide 4'-ether-alkylC4-acid		Alkyl	4	Acid
6917	Thalidomide 4'-ether-alkylC4-amine		Alkyl	4	Amine
7332	Thalidomide 4'-ether-alkylC5-acid		Alkyl	5	Acid
7522	Thalidomide 4'-ether-alkylC5-azide		Alkyl	5	Azide
6627	Thalidomide 4'-ether-alkylC6-amine		Alkyl	6	Amine
7333	Thalidomide 4'-ether-alkylC6-acid		Alkyl	6	Acid
7829	Thalidomide 4'-ether-alkylC6-azide		Alkyl	6	Azide
7334	Thalidomide 4'-ether-alkylC7-acid		Alkyl	7	Acid
7335	Thalidomide 4'-ether-alkylC8-acid		Alkyl	8	Acid
7403	Thalidomide 4'-ether-alkylC8-amine		Alkyl	8	Amine
7518	Thalidomide 4'-ether-PEG1-azide		PEG	1	Azide
6686	Thalidomide 4'-ether-PEG2-alkyne		PEG	2	Alkyne
7519	Thalidomide 4'-ether-PEG2-azide		PEG	2	Azide
6950	Thalidomide 4'-ether-PEG3-amine		PEG	3	Ethylamine
7520	Thalidomide 4'-ether-PEG3-azide		PEG	3	Azide
6951	Thalidomide 4'-ether-PEG5-amine		PEG	5	Ethylamine
6949	Thalidomide 4'-oxyacetamide-alkylC2-amine		Alkyl	2	Amine
6469	Thalidomide 4'-oxyacetamide-alkylC4-amine		Alkyl	4	Amine
6968	Thalidomide 4'-oxyacetamide-alkylC6-amine		Alkyl	6	Amine
6946	Thalidomide 4'-oxyacetamide-alkylC8-amine		Alkyl	2	Amine
6300	Thalidomide 4'-oxyacetamide-alkylC4-azide		Alkyl	4	Azide
6966	Thalidomide 4'-oxyacetamide-PEG1-amine		PEG	1	Ethylamine
6967	Thalidomide 4'-oxyacetamide-PEG2-amine		PEG	2	Ethylamine
6467	Thalidomide 4'-oxyacetamide-PEG3-amine		PEG	3	Amine
6468	Thalidomide 4'-oxyacetamide-PEG4-amine		PEG	4	Amine
6913	Thalidomide 4'-oxyacetamide-alkylC1-PEG3-alkylC3-amine		Alkyl-PEG-Alkyl	1-3-3	Amine
7988	Thalidomide 5'-amine-alkylc6-amine		Alkyl	6	Ethylamine
7557	Thalidomide 5'-amine-alkylc8-amine		Alkyl	8	Ethylamine
7733	Thalidomide 5'-amine-alkylC10-amine		Alkyl	10	Ethylamine
7735	Thalidomide 5'-amine-PEG1-amine		alkyl	10	Ethylamine
7736	Thalidomide 5'-amine-PEG2-amine		PEG	2	Ethylamine
7737	Thalidomide 5'-amine-PEG3-amine		PEG	3	Ethylamine

IAP Targeting Ligands Plus Linkers

Cat. No.	Product Name	Linker Type	Number of Units	Conjugation Functionality
6474	A 410099.1 amide-alkylC4-amine	Amide-Alkyl	4	Amine
6473	A 410099.1 amide-PEG2-amine	Amide-PEG	2	Amine
6472	A 410099.1 amide-PEG3-amine	Amide-PEG	3	Amine
7220	A 410099.1 amide-PEG4-amine	Amide-PEG	4	Amine
7221	A 410099.1 amide-PEG5-amine	Amide-PEG	5	Amine

Functionalized E3 Ligase Ligands

Cat. No.	Product Name	E3 Ligase Ligand	Target E3	Reactive Handle	Reaction Chemistry
8066	CST 530, Phenol	CST 530	IAP	Alcohol	Mitsunobu reaction
6471	A 410099.1, amine	A 410099.1	IAP	Primary Amine	Amide coupling
7178	LCL 161, phenol	LCL 161	IAP	Alcohol	Mitsunobu reaction
7677	Lenalidomide 5'-amine	Lenalidomide	Cereblon	Primary Amine	Amide Coupling
7858	PD 4'-oxyacetic acid	Phenyl Dihydrouracil	Cereblon	Carboxylic Acid	Amide Coupling
7859	PD 4'-piperazine	Phenyl Dihydrouracil	Cereblon	Cyclic Amine	Amide Coupling
7670	Phenyl-glutarimide 4'-oxyacetic acid	Phenyl-glutarimide	Cereblon	Carboxylic Acid	Amide Coupling
6466	TC E3 5031	Thalidomide	Cereblon	Carboxylic acid	Amide coupling
6628	TC E3 5032	Pomalidomide	Cereblon	Fluorine	Nucleophilic aromatic substitution
7456	Thalidomide, 5'-fluoro	Thalidomide	Cereblon	Fluoro	Nucleophilic aromatic substitution
6685	Thalidomide, propargyl	Thalidomide	Cereblon	Alkyne	Click chemistry
6462	VH 032, amine	VH 032	VHL	Primary amine	Amide coupling
6969	cis VH 032, amine dihydrochloride	VH 032	VHL	Primary amine	Amide coupling
7634	Me VH 032, amine	VH 032	VHL	Primary amine	Amide coupling
6911	VH 032, phenol	VH 032	VHL	Alcohol	Mitsunobu reaction
6683	VH 032, propargyl	VH 032	VHL	Alkyne	Click chemistry
7861	VH 032, thiol	VH 032	VHL	Thiol	Nucleophilic substitution
6952	VH 101, phenol	VH 101	VHL	Alcohol	Mitsunobu reaction
7884	VH 101, thiol	VH 101	VHL	Thiol	Nucleophilic substitution

Functionalized Warhead Ligands

Cat. No.	Product Name	Ligand	Target Protein	Reactive Handle	Reaction Chemistry
7689	(+)-JQ1 bump, acid functionalized	JQ1 analog	BET Bromodomains	Carboxylic acid	Amide coupling
6588	(+)-JQ1 carboxylic acid	JQ1	BET Bromodomains	Carboxylic acid	Amide coupling
7576	(+)-JQ1 maleimide	JQ1	BET Bromodomains	Maleimide	Sulfhydryl coupling
6589	(+)-JQ1 PA	JQ1	BET Bromodomains	Alkyne	Click chemistry

3. Negative Controls

Cat. No.	Product	Activity
7255	ARCC 4 negative control	Negative control for ARCC 4 (Cat. No. 7254)
7529	BSJ-4-116-NC	Negative control for BSJ-4-116 (Cat. No. 7528)
7426	CG 428-Neg	Negative control for CG 428 (Cat. No. 7425)
7428	CG 858-Neg	Negative control for CG 858 (Cat. No. 7427)
6155	cis MZ 1	Negative Control for MZ 1 (Cat. No. 6154)
7433	cis-SIM1	Negative control for SIM1 (Cat. No. 7432)
6939	cis-VZ 185	Negative control for VZ 185 (Cat. No. 6936)
8084	JPS016NC	Negative control for JPS036 (Cat. No. 8085).
7421	LC 2 Epimer	Negative control for LC 2 (Cat. No. 7420)
7504	MD15	Negative control for MD13 (Cat. No. 7503)
7396	MS 154N	Negative control for MS 154 (Cat No. 7395)
7398	MS 39N	Negative control for MS 39 (Cat. No. 7397)
8005	PROTAC®(H-PGDS)-8	Negative control for PROTAC®(H-PGDS)-7 (Cat. No. 8004)
7464	SJF 0661	Negative control for SJF 0628 (Cat. No. 7463)
7588	SK 575-NEG	Negative control for SK 575 (Cat. No. 7583)
8054	STING Degrader N-Me-SP23	Negative control for STING Degrader SP23 (Cat. No. 8053)
7260	TBK1 control PROTAC® 4	Negative control for TBK1 PROTAC® 3i (Cat. No. 7259)
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)
8041	α-Synuclein Degrader 2bn	Negative control for α Synuclein Degrader 2b (Cat. No. 8040)

주문정보

주문정보 - Cat No, PRODUCT, SIZE, 수량 등 항목으로 구성되어있습니다.
Product	Cat.No.	Size	Maker
PD 4'-oxyacetic acid	7858	50 mg	TOCRIS
NX 2127	8951	5 mg	TOCRIS
(+)-JQ1 bump, acid functionalized	7689	50 mg	TOCRIS
(+)-JQ1 bump-N, acid functionalized	8827	25 mg	TOCRIS
(+)-JQ1 maleimide	7576	10 mg	TOCRIS
5-Amino-Thalidomide	7678	100 mg	TOCRIS
5-Ph-IAA-AM	7893	10 mg	TOCRIS
5-Ph-IAA-AM	7893	50 mg	TOCRIS
A 410099.1 amide-alkylC4-amine (25 MG)	6474	25 mg	TOCRIS
A 410099.1 amide-PEG2-amine (25 MG)	6473	25 mg	TOCRIS
A 410099.1 amide-PEG3-amine (25 MG)	6472	25 mg	TOCRIS
A 410099.1 amide-PEG4-amine (25 MG)	7220	25 mg	TOCRIS
A 410099.1 amide-PEG5-amine (25 MG)	7221	25 mg	TOCRIS
A 410099.1, amine (100 MG)	6471	100 mg	TOCRIS
a-Synuclein Degrader 2b	8040	5 mg	TOCRIS
a-Synuclein Degrader 2bn	8041	5 mg	TOCRIS
a-Synuclein Degrader 2bn	8041	5 mg	TOCRIS
a1A-AR Degrader 9c	7278	5 mg	TOCRIS
Active Degraders	8118	5 mg	TOCRIS
AP 1867	6207	10 mg	TOCRIS
AP 1867	6207	50 mg	TOCRIS
ARCC 4 negative control (5 MG)	7255	5 mg	TOCRIS
ARV 771 (5 MG)	7256	5 MG	TOCRIS
AT 1 (5 MG)	6356	5 mg	TOCRIS
AUTAC4	7699	5 mg	TOCRIS
AZ 3137	8833	5 mg	TOCRIS
BRD PHOTAC-I-3 (5 mg)	7319	5 mg	TOCRIS
BSJ-03-123 (5 MG)	6921	5 mg	TOCRIS
BSJ-03-204 (5 MG)	6938	5 mg	TOCRIS
BSJ-04-132 (5 MG)	6937	5 mg	TOCRIS
BSJ-4-116	7528	5 mg	TOCRIS
BSJ-4-116-NC	7529	5 mg	TOCRIS
CG 428	7425	5 mg	TOCRIS
CG 428-Neg	7426	5 mg	TOCRIS
CG 858	7427	5 mg	TOCRIS
CG 858-Neg	7428	5 mg	TOCRIS
cis MZ 1 (5 MG)	6155	5 mg	TOCRIS
cis VH 032, amine dihydrochloride (50 MG)	6969	50 mg	TOCRIS
cis-SIM1	7433	2 mg	TOCRIS
cis-VZ 185 (5 MG)	6939	5 mg	TOCRIS
CM 11 (5 MG)	6416	5 mg	TOCRIS
CPS2	7800/2	2 mg	TOCRIS
CRBN PROTAC 14a (5 MG)	7219	5 mg	TOCRIS
CRBN-6-5-5-VHL (5 MG)	6948	5 mg	TOCRIS
CSN5i-3-NEG	7532	2 mg	TOCRIS
CST 530, Phenol	8066	50 mg	TOCRIS
CST 626	8021	2 mg	TOCRIS
CST 905	7745	5 mg	TOCRIS
CST 967	7801	5 mg	TOCRIS
dBET1 (5 MG)	6327	5 mg	TOCRIS

전체보기

1
Maker	TOCRIS
Cat.No.	7858
Product	PD 4'-oxyacetic acid
Size	50 mg
Qty
Data Sheet
MSDS

2
Maker	TOCRIS
Cat.No.	8951
Product	NX 2127
Size	5 mg
Qty
MSDS

3
Maker	TOCRIS
Cat.No.	7689
Product	(+)-JQ1 bump, acid functionalized
Size	50 mg
Qty
Data Sheet
MSDS

4
Maker	TOCRIS
Cat.No.	8827
Product	(+)-JQ1 bump-N, acid functionalized
Size	25 mg
Qty
Data Sheet
MSDS

5
Maker	TOCRIS
Cat.No.	7576
Product	(+)-JQ1 maleimide
Size	10 mg
Qty
Data Sheet
MSDS

6
Maker	TOCRIS
Cat.No.	7678
Product	5-Amino-Thalidomide
Size	100 mg
Qty
Data Sheet
MSDS

7
Maker	TOCRIS
Cat.No.	7893
Product	5-Ph-IAA-AM
Size	10 mg
Qty
Data Sheet
MSDS

8
Maker	TOCRIS
Cat.No.	7893
Product	5-Ph-IAA-AM
Size	50 mg
Qty
Data Sheet
MSDS

9
Maker	TOCRIS
Cat.No.	6474
Product	A 410099.1 amide-alkylC4-amine (25 MG)
Size	25 mg
Qty
Data Sheet
MSDS

10
Maker	TOCRIS
Cat.No.	6473
Product	A 410099.1 amide-PEG2-amine (25 MG)
Size	25 mg
Qty
Data Sheet
MSDS

11
Maker	TOCRIS
Cat.No.	6472
Product	A 410099.1 amide-PEG3-amine (25 MG)
Size	25 mg
Qty
Data Sheet
MSDS

12
Maker	TOCRIS
Cat.No.	7220
Product	A 410099.1 amide-PEG4-amine (25 MG)
Size	25 mg
Qty
Data Sheet
MSDS

13
Maker	TOCRIS
Cat.No.	7221
Product	A 410099.1 amide-PEG5-amine (25 MG)
Size	25 mg
Qty
Data Sheet
MSDS

14
Maker	TOCRIS
Cat.No.	6471
Product	A 410099.1, amine (100 MG)
Size	100 mg
Qty
Data Sheet
MSDS

15
Maker	TOCRIS
Cat.No.	8040
Product	a-Synuclein Degrader 2b
Size	5 mg
Qty
Data Sheet
MSDS

16
Maker	TOCRIS
Cat.No.	8041
Product	a-Synuclein Degrader 2bn
Size	5 mg
Qty
Data Sheet
MSDS

17
Maker	TOCRIS
Cat.No.	8041
Product	a-Synuclein Degrader 2bn
Size	5 mg
Qty
Data Sheet
MSDS

18
Maker	TOCRIS
Cat.No.	7278
Product	a1A-AR Degrader 9c
Size	5 mg
Qty
Data Sheet
MSDS

19
Maker	TOCRIS
Cat.No.	8118
Product	Active Degraders
Size	5 mg
Qty
Data Sheet
MSDS

20
Maker	TOCRIS
Cat.No.	6207
Product	AP 1867
Size	10 mg
Qty
Data Sheet
MSDS

21
Maker	TOCRIS
Cat.No.	6207
Product	AP 1867
Size	50 mg
Qty
Data Sheet
MSDS

22
Maker	TOCRIS
Cat.No.	7255
Product	ARCC 4 negative control (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

23
Maker	TOCRIS
Cat.No.	7256
Product	ARV 771 (5 MG)
Size	5 MG
Qty
Data Sheet
MSDS

24
Maker	TOCRIS
Cat.No.	6356
Product	AT 1 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

25
Maker	TOCRIS
Cat.No.	7699
Product	AUTAC4
Size	5 mg
Qty
Data Sheet
MSDS

26
Maker	TOCRIS
Cat.No.	8833
Product	AZ 3137
Size	5 mg
Qty
Data Sheet
MSDS

27
Maker	TOCRIS
Cat.No.	7319
Product	BRD PHOTAC-I-3 (5 mg)
Size	5 mg
Qty
Data Sheet
MSDS

28
Maker	TOCRIS
Cat.No.	6921
Product	BSJ-03-123 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

29
Maker	TOCRIS
Cat.No.	6938
Product	BSJ-03-204 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

30
Maker	TOCRIS
Cat.No.	6937
Product	BSJ-04-132 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

31
Maker	TOCRIS
Cat.No.	7528
Product	BSJ-4-116
Size	5 mg
Qty
Data Sheet
MSDS

32
Maker	TOCRIS
Cat.No.	7529
Product	BSJ-4-116-NC
Size	5 mg
Qty
Data Sheet
MSDS

33
Maker	TOCRIS
Cat.No.	7425
Product	CG 428
Size	5 mg
Qty
Data Sheet
MSDS

34
Maker	TOCRIS
Cat.No.	7426
Product	CG 428-Neg
Size	5 mg
Qty
Data Sheet
MSDS

35
Maker	TOCRIS
Cat.No.	7427
Product	CG 858
Size	5 mg
Qty
Data Sheet
MSDS

36
Maker	TOCRIS
Cat.No.	7428
Product	CG 858-Neg
Size	5 mg
Qty
Data Sheet
MSDS

37
Maker	TOCRIS
Cat.No.	6155
Product	cis MZ 1 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

38
Maker	TOCRIS
Cat.No.	6969
Product	cis VH 032, amine dihydrochloride (50 MG)
Size	50 mg
Qty
Data Sheet
MSDS

39
Maker	TOCRIS
Cat.No.	7433
Product	cis-SIM1
Size	2 mg
Qty
Data Sheet
MSDS

40
Maker	TOCRIS
Cat.No.	6939
Product	cis-VZ 185 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

41
Maker	TOCRIS
Cat.No.	6416
Product	CM 11 (5 MG)
Size	5 mg
Qty
Data Sheet
MSDS

전체보기

자료

표적 단백질 분해 PRODUCT GUIDE

[TOCRIS]

Targeted Protein Degradation에 대한 PRODUCT GUIDE 한글판 입니다.
Targeted Protein Degradation Research Product Guide

[TOCRIS]

PROTAC 연구에 필요한 linker 및 degrader를 제공합니다.
Advance Emerging Therapeutics for Undruggable Targets

[EUROFINS DISCOVERX]

PROTAC을 이용한 Targeted Protein Degradation Drug Discovery Solutions을 안내합니다.
Targeted Protein Degradation Assays

[EUROFINS DISCOVERX]

PROTAC에 의해 유도된 Protein의 turnover를 측정하기 위한 assay platform에 대한 안내입니다.
Inhibitor Book Vol.4

[고마바이오텍]

다양한 Disease 및 pathway 에 관련된 inhibitor 자료 입니다.

웨비나/Video

[TOCRIS] Tools for Targeted Protein Degradation

PROTAC 기술에 대한 안내 영상입니다.

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

PROTAC 기술에 대한 안내입니다.

동영상 보기
[TOCRIS] dTAG - A Powerful New Tag-Based Degradation System

dTAG 기술에 대한 안내입니다.

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

PROTAC 스크리닝에 대한 웨비나 입니다.

동영상 보기